Category: 630125-91-6

Huang, Wei-Sheng et al. published their research in Journal of Medicinal Chemistry in 2010 | CAS: 630125-91-6

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-[4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl]benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant was written by Huang, Wei-Sheng;Metcalf, Chester A.;Sundaramoorthi, Raji;Wang, Yihan;Zou, Dong;Thomas, R. Mathew;Zhu, Xiaotian;Cai, Lisi;Wen, David;Liu, Shuangying;Romero, Jan;Qi, Jiwei;Chen, Ingrid;Banda, Geetha;Lentini, Scott P.;Das, Sasmita;Xu, Qihong;Keats, Jeff;Wang, Frank;Wardwell, Scott;Ning, Yaoyu;Snodgrass, Joseph T.;Broudy, Marc I.;Russian, Karin;Zhou, Tianjun;Commodore, Lois;Narasimhan, Narayana I.;Mohemmad, Qurish K.;Iuliucci, John;Rivera, Victor M.;Dalgarno, David C.;Sawyer, Tomi K.;Clackson, Tim;Shakespeare, William C.. And the article was included in Journal of Medicinal Chemistry in 2010.Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline This article mentions the following:

In the treatment of chronic myeloid leukemia (CML) with BCR-ABL kinase inhibitors, the T315I gatekeeper mutant has emerged as resistant to all currently approved agents. This report describes the structure-guided design of a novel series of potent pan-inhibitors of BCR-ABL, including the T315I mutation. A key structural feature is the carbon-carbon triple bond linker which skirts the increased bulk of Ile315 side chain. Extensive SAR studies led to the discovery of development candidate benzamide I (AP24534), which inhibited the kinase activity of both native BCR-ABL and the T315I mutant with low nM IC50s, and potently inhibited proliferation of corresponding Ba/F3-derived cell lines. Daily oral administration of I significantly prolonged survival of mice injected i.v. with BCR-ABLT315I expressing Ba/F3 cells. These data, coupled with a favorable ADME profile, support the potential of I to be an effective treatment for CML, including patients refractory to all currently approved therapies. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Furukawa, Takenori et al. published their research in ACS Medicinal Chemistry Letters in 2021 | CAS: 630125-91-6

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. COA of Formula: C14H20F3N3

A Putative Single-Photon Emission CT Imaging Tracer for Erythropoietin-Producing Hepatocellular A2 Receptor was written by Furukawa, Takenori;Kimura, Hiroyuki;Torimoto, Hanae;Yagi, Yusuke;Kawashima, Hidekazu;Arimitsu, Kenji;Yasui, Hiroyuki. And the article was included in ACS Medicinal Chemistry Letters in 2021.COA of Formula: C14H20F3N3 This article mentions the following:

Erythropoietin-producing hepatocellular (Eph) receptors are receptor tyrosine kinases involved in cell-cell contact. The EphA2 receptor is associated with cancer proliferation and migration. Therefore, EphA2 receptor imaging has the potential for cancer diagnosis. Here, we synthesized N-(5-((4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)-2-methylphenyl)-5-[123I]iodonicotinamide ([123I]ETB) and evaluated it as an imaging tracer for single-photon emission computed tomog. (SPECT) imaging of the EphA2 receptor. [123I]ETB was designed on the basis of ALW-II-41-27, an inhibitor of EphA2 receptor kinase. Nonradioactive ETB was also synthesized and has been shown to efficiently inhibit EphA2 receptor kinase activity in vitro (IC50: ETB, 90.2 ± 18.9 nM). A cell-binding assay demonstrated that [125I]ETB binds specifically to the EphA2 receptor. The ex vivo biodistribution study of [125I]ETB in U87MG tumor-bearing mice also revealed tumor uptake (2.2% ID/g at 240 min). In addition, [123I]ETB uptake in tumors was visualized via SPECT/CT imaging. On the basis of the above, [123I]ETB can be considered a potential SPECT imaging tracer for the EphA2 receptor. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6COA of Formula: C14H20F3N3).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. COA of Formula: C14H20F3N3

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Huang, Wei-Sheng et al. published their research in Journal of Medicinal Chemistry in 2010 | CAS: 630125-91-6

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-[4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl]benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant was written by Huang, Wei-Sheng;Metcalf, Chester A.;Sundaramoorthi, Raji;Wang, Yihan;Zou, Dong;Thomas, R. Mathew;Zhu, Xiaotian;Cai, Lisi;Wen, David;Liu, Shuangying;Romero, Jan;Qi, Jiwei;Chen, Ingrid;Banda, Geetha;Lentini, Scott P.;Das, Sasmita;Xu, Qihong;Keats, Jeff;Wang, Frank;Wardwell, Scott;Ning, Yaoyu;Snodgrass, Joseph T.;Broudy, Marc I.;Russian, Karin;Zhou, Tianjun;Commodore, Lois;Narasimhan, Narayana I.;Mohemmad, Qurish K.;Iuliucci, John;Rivera, Victor M.;Dalgarno, David C.;Sawyer, Tomi K.;Clackson, Tim;Shakespeare, William C.. And the article was included in Journal of Medicinal Chemistry in 2010.Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline This article mentions the following:

In the treatment of chronic myeloid leukemia (CML) with BCR-ABL kinase inhibitors, the T315I gatekeeper mutant has emerged as resistant to all currently approved agents. This report describes the structure-guided design of a novel series of potent pan-inhibitors of BCR-ABL, including the T315I mutation. A key structural feature is the carbon-carbon triple bond linker which skirts the increased bulk of Ile315 side chain. Extensive SAR studies led to the discovery of development candidate benzamide I (AP24534), which inhibited the kinase activity of both native BCR-ABL and the T315I mutant with low nM IC50s, and potently inhibited proliferation of corresponding Ba/F3-derived cell lines. Daily oral administration of I significantly prolonged survival of mice injected i.v. with BCR-ABLT315I expressing Ba/F3 cells. These data, coupled with a favorable ADME profile, support the potential of I to be an effective treatment for CML, including patients refractory to all currently approved therapies. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Canning, Peter et al. published their research in Journal of Molecular Biology in 2014 | CAS: 630125-91-6

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Computed Properties of C14H20F3N3

Structural Mechanisms Determining Inhibition of the Collagen Receptor DDR1 by Selective and Multi-Targeted Type II Kinase Inhibitors was written by Canning, Peter;Tan, Li;Chu, Kiki;Lee, Sam W.;Gray, Nathanael S.;Bullock, Alex N.. And the article was included in Journal of Molecular Biology in 2014.Computed Properties of C14H20F3N3 This article mentions the following:

The discoidin domain receptors (DDRs), DDR1 and DDR2, form a unique subfamily of receptor tyrosine kinases that are activated by the binding of triple-helical collagen. Excessive signaling by DDR1 and DDR2 has been linked to the progression of various human diseases, including fibrosis, atherosclerosis and cancer. The authors report the inhibition of these unusual receptor tyrosine kinases by the multi-targeted cancer drugs imatinib and ponatinib, as well as the selective type II inhibitor DDR1-IN-1. Ponatinib is identified as the more potent mol., which inhibits DDR1 and DDR2 with an IC50 of 9 nM. Co-crystal structures of human DDR1 reveal a DFG-out conformation (DFG, Asp-Phe-Gly) of the kinase domain that is stabilized by an unusual salt bridge between the activation loop and αD helix. Differences to Abelson kinase (ABL) are observed in the DDR1 P-loop, where a β-hairpin replaces the cage-like structure of ABL. P-loop residues in DDR1 that confer drug resistance in ABL are therefore accommodated outside the ATP pocket. Whereas imatinib and ponatinib bind potently to both the DDR and ABL kinases, the hydrophobic interactions of the ABL P-loop appear poorly satisfied by DDR1-IN-1 suggesting a structural basis for its DDR1 selectivity. Such inhibitors may have applications in clin. indications of DDR1 and DDR2 overexpression or mutation, including lung cancer. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Computed Properties of C14H20F3N3).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Computed Properties of C14H20F3N3

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Cherian, Joseph et al. published their research in Journal of Medicinal Chemistry in 2016 | CAS: 630125-91-6

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Name: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells was written by Cherian, Joseph;Nacro, Kassoum;Poh, Zhi Ying;Guo, Samantha;Jeyaraj, Duraiswamy A.;Wong, Yun Xuan;Ho, Melvyn;Yang, Hai Yan;Joy, Joma Kanikadu;Kwek, Zekui Perlyn;Liu, Boping;Wee, John Liang Kuan;Ong, Esther HQ;Choong, Meng Ling;Poulsen, Anders;Lee, May Ann;Pendharkar, Vishal;Ding, Li Jun;Manoharan, Vithya;Chew, Yun Shan;Sangthongpitag, Kanda;Lim, Sharon;Ong, S. Tiong;Hill, Jeffrey;Keller, Thomas H.. And the article was included in Journal of Medicinal Chemistry in 2016.Name: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline This article mentions the following:

Clin. used BCR-ABL1 inhibitors for the treatment of chronic myeloid leukemia do not eliminate leukemic stem cells (LSC). It has been shown that MNK1 and 2 inhibitors prevent phosphorylation of eIF4E and eliminate the self-renewal capacity of LSCs. Herein, the authors describe the identification of novel dual MNK1 and 2 and BCR-ABL1 inhibitors, starting from the known kinase inhibitor. Initial structure-activity relationship studies resulted in a compound with loss of BCR-ABL1 inhibition. Further modification led to orally bioavailable dual MNK1 and 2 and BCR-ABL1 inhibitors I and II, which are efficacious in a mouse xenograft model and also reduce the level of phosphorylated eukaryotic translation initiation factor 4E in the tumor tissues. Kinase selectivity of these compounds is also presented. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Name: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Name: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Liang, Xiaofei et al. published their research in Journal of Medicinal Chemistry in 2019 | CAS: 630125-91-6

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

Discovery of N-(4-(6-acetamidopyrimidin-4-yloxy)phenyl)-2-(2-(trifluoromethyl)phenyl)acetamide (CHMFL-FLT3-335) as a potent FMS-like tyrosine kinase 3 internal tandem duplication (FLT3-ITD) mutant selective inhibitor for acute myeloid leukemia was written by Liang, Xiaofei;Wang, Beilei;Chen, Cheng;Wang, Aoli;Hu, Chen;Zou, Fengming;Yu, Kailin;Liu, Qingwang;Li, Feng;Hu, Zhenquan;Lu, Tingting;Wang, Junjie;Wang, Li;Weisberg, Ellen L.;Li, Lili;Xia, Ruixiang;Wang, Wenchao;Ren, Tao;Ge, Jian;Liu, Jing;Liu, Qingsong. And the article was included in Journal of Medicinal Chemistry in 2019.Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline This article mentions the following:

Most of the current FMS-like tyrosine kinase 3 (FLT3) inhibitors lack selectivity between FLT3 kinase and cKIT kinase as well as the FLT3 wt and internal tandem duplication (ITD) mutants. We report a new compound I, which displays GI50 values of 30-80 nM against different ITD mutants and achieves selectivity over both FLT3 wt (8-fold) and cKIT kinase in the transformed BaF3 cells (>300-fold). I potently inhibits the proliferation of the FLT3-ITD-pos. acute myeloid leukemia cancer lines through suppression of the phosphorylation of FLT3 kinase and downstream signaling pathways, induction of apoptosis, and arresting the cell cycle into the G0/G1 phase. I also displays potent antiproliferative effect against FLT3-ITD-pos. patient primary cells, whereas it does not apparently affect FLT3 wt primary cells. In addition, it also exhibits a good therapeutic window to PBMC compared to PKC412. In the in vivo studies, I demonstrates favorable PK profiles and suppresses the tumor growth in the MV4-11 cell inoculated mouse xenograft model. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Recommanded Product: 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Weir, Mark C. et al. published their research in ACS Chemical Biology in 2018 | CAS: 630125-91-6

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Category: piperazines

Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo was written by Weir, Mark C.;Shu, Sherry T.;Patel, Ravi K.;Hellwig, Sabine;Chen, Li;Tan, Li;Gray, Nathanael S.;Smithgall, Thomas E.. And the article was included in ACS Chemical Biology in 2018.Category: piperazines This article mentions the following:

Acute myelogenous leukemia (AML) is the most common hematol. malignancy in adults and is often associated with constitutive tyrosine kinase signaling. These pathways involve the nonreceptor tyrosine kinases Fes, Syk, and the three Src-family kinases expressed in myeloid cells (Fgr, Hck, and Lyn). In this study, we report remarkable anti-AML efficacy of an N-phenylbenzamide kinase inhibitor, TL02-59. This compound potently suppressed the proliferation of bone marrow samples from 20 of 26 AML patients, with a striking correlation between inhibitor sensitivity and expression levels of the myeloid Src family kinases Fgr, Hck, and Lyn. No correlation was observed with Flt3 expression or mutational status, with the four most sensitive patient samples being wild-type for Flt3. Kinome-wide target specificity profiling coupled with in vitro kinase assays demonstrated a narrow overall target specificity profile for TL02-59, with picomolar potency against the myeloid Src-family member Fgr. In a mouse xenograft model of AML, oral administration of TL02-59 for 3 wk at 10 mg/kg completely eliminated leukemic cells from the spleen and peripheral blood while significantly reducing bone marrow engraftment. These results identify Fgr as a previously unrecognized kinase inhibitor target in AML and TL02-59 as a possible lead compound for clin. development in AML cases that overexpress this kinase independent of Flt3 mutations. In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Category: piperazines).

4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

27 Sep 2021 News Downstream synthetic route of 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

630125-91-6, 630125-91-6 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 59134564, apiperazines compound, is more and more widely used in various fields.

630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 3-(2-(cyclopropanecarboxamido)thiazolo[5,4-b]pyridin-5-yl) benzoic acid (150 mg, 0.44 mmol) and triethylamine (90 muL, 0.66 mmol) in toluene (2 niL) was added diphenylphosphoryl azide (0.11 niL, 0.49 mmol). The resulting mixture was stirred at room temperature for 30 minutes and heated at 80 0C for 1 h. To a reaction mixture was added 4-((4-ethylpiperazin-l-yl)methyl)-3-(trifluoromethyl) aniline (121 mg, 0.42 mmol) and triethylamine (90 muL, 0.66 mmol). The reaction mixture was stirred at 80 0C for 2h and most of organic solvent was removed in vacuo. The crude product was diluted with DMSO (3 mL) and purified by preparative HPLC to give the title compound as a TFA salt.1H NMR 600 MHz (CDCl3) delta 8.51 (s, IH), 7.83 (d, J= 1.8 Hz, IH), 7.48 (m, 2H), 7.19 (m, 3H), 7.12 (m, 2H), 6.85 (J, J= 3.0 Hz, IH), 6.49 (m, IH), 6.19 (m, 2H), 3.84 (m, IH), 3.78 (s, 3H), 3.46 (m, 2H), 3.19 (m, IH), 2.90 (m, 2H), 1.99 (m, 2H), 1.69 (m, 2H), 1.19 (J, J= 6.6 Hz, 6H), MS m/z : 624.36 (M + 1).

630125-91-6, 630125-91-6 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 59134564, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; NOVARTIS AG; CHOI, Hwan, Geun; SIM, Taebo; GRAY, Nathanael; ZHOU, Wenjun; CHANG, Jae, Won; ZHANG, Jianming; WEISBERG, Ellen; WO2010/144909; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

22 Sep 2021 News Analyzing the synthesis route of 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

630125-91-6, To a solution of 4- ( (4-ethylpiperazin-1-yl) methyl) -3- (trifluoromethyl) aniline (60 mg 0.209 mmol) in THF (10 mL) was added triphosgene (21.69 mg 0.073 mmol) . The resulting mixture was stirred at 70 . After 30 min TLC analysis (PE/EA 3/1) showed the starting material was disappeared. The solvent was removed in vacuo to give a brown oil of 1-ethyl-4- (4-isocyanato-2- (trifluoromethyl) benzyl) piperazine (65 mg 0.197 mmol 94yield) . To a solution of 4- ( (5-ethoxy-6- ( (4-methoxybenzyl) oxy) pyridin-3-yl) oxy) aniline (50 mg 0.136 mmol) and Et3N (44 mg 0.4 mmol) in THF (10 mL) was added a solution of 1-ethyl-4- (4-isocyanato-2- (trifluoromethyl) benzyl) piperazine (64.1 mg 0.205 mmol) in THF (10 mL) . The resulting mixture was stirred at 70 . After LCMS analysis showed the starting material was disappeared. The solvent was removed in vacuo. The residue was washed with H2O. The residue was purified by preparative TLC to yield a white solid of 1- (4- ( (5-ethoxy-6- ( (4-methoxybenzyl) oxy) pyridin-3-yl) oxy) phenyl) -3- (4- ( (4-ethylpiperazin-1-yl) methyl) -3- (trifluoromethyl) phenyl) urea (50 mg 0.070 mmol 51.2yield) 1HNMR(400 MHz CD3OD) delta 7.85 (d J 2.0 Hz 1H) 7.66-7.64 (m 2H) 7.42-7.36 (m 5H) 6.99-6.95 (m 3H) 6.89 (dd J 6.8 2.0 Hz 2H) 5.29 (s 2H) 4.03-3.98 (m 2H) 3.79 (s 3H) 3.69 (s 2H) 3.31-2.65 (m 8H) 1.37 (t J 7.0 Hz 3H) 1.27 (t J 7.2 Hz 3H) ES-LCMS m/z 680.1 (M+H) .

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXOSMITHKLINE (CHINA) R & D COMPANY LIMITED; CHEUNG, Mui; DEMARTINO, Michael P.; EIDAM, Hilary Schenck; GUAN, Huiping Amy; QIN, Donghui; WU, Chengde; GONG, Zhen; YANG, Haiying; YU, Haiyu; ZHANG, Zhiliu; (391 pag.)WO2016/37578; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

15 Sep 2021 News Analyzing the synthesis route of 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

630125-91-6,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

To a suspension of triphosgene (0.21 g, 0.71 mmol) and Na2C03 (0.45 g, 4.27 mmol) in DCM (18 ml), kept at 0 ocunder argon, 4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine (0.61 g, 2.13 mmol) was added. Thereaction was monitored by HPLC (following the formation of 4-ethyl-piperazine-1-carboxylic acid [4-(4-ethylpiperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-amide by treating a sample of the reaction mixture with N-25 ethylpiperazine). After 1 h, 3-ethynyl-phenylamine (0.26 g, 2.18 mmol) was added and the reaction was let understirring overnight at r.t.. The mixture was diluted with DCM, washed with water (3 x 10 ml), dried over anhydrousNa2S04 and concentrated under vacuum. Purification by flash column chromatography (DCM/MeOH 95/5) affordedthe product as yellow solid (0.64 g, 70%).1H NMR (600 MHz, DMSO-dG) o ppm 0.95-1.00 (m, 3 H) 2.22-2.47 (m, 10 H) 3.52 (s, 2 H) 4.14 (s, 1 H) 7.09 (d,30 J=7.69 Hz, 1 H) 7.30 (t, J=7.88 Hz, 1 H) 7.41 (dd, J=8.24, 1.28 Hz, 1 H) 7.56 (dd, J=8.61, 1.83 Hz, 1 H) 7.61 – 7.64(m, 1 H) 7.66 (t, J=1.65 Hz, 1 H) 7.95 (d, J=2.01 Hz, 1 H) 8.85 (s, 1 H) 9.02 (s, 1 H).

As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.

Reference：
Patent; NERVIANO MEDICAL SCIENCES S.R.L.; MENICHINCHERI, Maria; ANGIOLINI, Mauro; BERTRAND, Jay Aaron; CARUSO, Michele; POLUCCI, Paolo; QUARTIERI, Francesca; SALOM, Barbara; SALSA, Matteo; ZUCCOTTO, Fabio; WO2014/72220; (2014); A1;,
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