Month: January 2023

A novel co-production process for piperazine and its N-monoalkyl derivatives was written by Wu, Zhiwei;Wang, Huabang;Sun, Meng;Du, Xiaobao;Chen, Ligong;Li, Yang. And the article was included in Research on Chemical Intermediates in 2012.Product Details of 21867-64-1 This article mentions the following:

A novel co-production process for piperazine and its N-monoalkyl derivatives has been established. N-β-hydroxyethyl-1,2-ethylenediamine and alcs. were used as the starting materials and the process was carried out over Cu-Cr-La/γ-Al₂O₃ in a fixed-bed reactor. Alcs. acted not only as the solvent but also as the alkylating reagent. The catalyst was characterized by XRD, XPS and BET. The results obtained showed that Cu⁰ particles in the catalyst were the active sites and doping with La led to enhancement of catalyst activity. Process conditions including reaction temperature, hydrogen pressure, and molar ratio of the reagents were optimized and the distribution of the products was found to be markedly dependent on reaction temperature Using optimum conditions, piperazine and its N-monoalkyl derivatives were obtained with satisfactory yields and distributions. The catalyst performed well for over 300 h. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Product Details of 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) 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. 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.Product Details of 21867-64-1

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

Studies on the compounds related to azulene. I. Synthesis and antiallergic activity of guaiazulenylglyoxylamides, guaiazulenylglyoxylic acid esters and acylaminoguaiazulenes was written by Hamajima, Ryo;Iwano, Katsuyuki;Okuda, Hirohisa. And the article was included in Yakugaku Zasshi in 1978.Name: 1-Propylpiperazine This article mentions the following:

New guaiazulenylglyoxylamides, guaiazulenglyoxylic acid esters, guaiazulenylglyoxypiperazines, and acylaminoguaiazulenes were prepared, and their antiallergic activities were evaluated by passive cutaneous anaphylaxis (PCA) test in the rat. Guaiazulenylglyoxalyl chloride I (R = Cl) derived from guaiazulene and oxalyl chloride was converted into glyoxylamides, glyoxylic acid esters, and glyoxylpiperazines with appropriate amines, alcs., and piperazines. Acylaminoguaiazulenes were prepared from 3-aminoguaiazulene with the corresponding acid anhydride or acid chloride. Many of guaiazulenylglyoxylpiperazines, especially I (R = 4-R¹-piperazin-1-yl; R¹ = H, Me, Et, CH₂CO₂H, PhCH₂) showed a high antiallergic activity by oral administration, but none of the other types of compounds showed a significant activity. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Name: 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Name: 1-Propylpiperazine

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

Synthesis of substituted 4-oxo-7-sulfamoyl-2,3,4,5-tetrahydrobenzo[b][1,4]thiazepines was written by Kravchenko, D. V.;Ivanovskii, S. A.;Korsakov, M. K.;Dorogov, M. V.;Tkachenko, S. E.;AsHchenko, A. V.. And the article was included in Izvestiya Vysshikh Uchebnykh Zavedenii, Khimiya i Khimicheskaya Tekhnologiya in 2005.COA of Formula: C13H21N3 This article mentions the following:

A combinatorial library of substituted 4-oxo-7-sulfamoyl-2,3,4,5-tetrahydrobenzo[b][1,4]thiazepines was synthesized via chlorosulfonylation of tetrahydrobenzothiazepinones followed by reaction with a range of primary and secondary amines. Physicochem. parameters of some of the products, such as lipophilicity, number of rotating bonds and number of hydrogen bond donors and acceptors have been calculated In the experiment, the researchers used many compounds, for example, 4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6COA of Formula: C13H21N3).

4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.COA of Formula: C13H21N3

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

The discovery of potent antagonists of NPBWR1 (GPR7) was written by Romero, F. Anthony;Hastings, Nicholas B.;Moningka, Remond;Guo, Zhiqiang;Wang, Ming;Di Salvo, Jerry;Lei, Ying;Trusca, Dorina;Deng, Qiaolin;Tong, Vincent;Terebetski, Jenna L.;Ball, Richard G.;Ujjainwalla, Feroze. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Synthetic Route of C10H12N4 This article mentions the following:

The synthesis and evaluation of small mol. antagonists of the G protein-coupled receptor NPBWR1 (GPR7) are reported for the first time. [4-(5-Chloropyridin-2-yl)piperazin-1-yl][(1S,2S,4R)-4-{[(1R)-1-(4-methoxyphenyl)ethyl]amino}-2-(thiophen-3-yl)cyclohexyl]methanone (I) emerged as a hit from a high-throughput screen. Examination of substituents that focused on replacing the 5-chloropyridine and 4-methoxybenzylamino groups of I led to the identification of compounds that exhibited subnanomolar potencies as low as 660 pM {II [X = NH]} in the functional assay and 200 pM in the binding assay {II [X = O]}. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Synthetic Route of C10H12N4).

6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Synthetic Route of C10H12N4

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

Catalytic C(sp³)-H bond activation in tertiary alkylamines was written by Rodrigalvarez, Jesus;Nappi, Manuel;Azuma, Hiroki;Floden, Nils J.;Burns, Matthew E.;Gaunt, Matthew J.. And the article was included in Nature Chemistry in 2020.Name: 1-Propylpiperazine This article mentions the following:

The development of robust catalytic methods to assemble tertiary alkylamines provides a continual challenge to chem. synthesis. In this regard, transformation of a traditionally unreactive C-H bond, proximal to the nitrogen atom, into a versatile chem. entity would be a powerful strategy for introducing functional complexity to tertiary alkylamines. A practical and selective metal-catalyzed C(sp³)-H activation facilitated by the tertiary alkylamine functionality, however, remains an unsolved problem. Here, we report a Pd(II)-catalyzed protocol that appends arene feedstocks to tertiary alkylamines via C(sp³)-H functionalization. A simple ligand for Pd(II) orchestrates the C-H activation step in favor of deleterious pathways. The reaction can use both simple and complex starting materials to produce a range of multifaceted γ-aryl tertiary alkylamines and can be rendered enantioselective. The enabling features of this transformation should be attractive to practitioners of synthetic and medicinal chem. as well as in other areas that use biol. active alkylamines. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Name: 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) 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. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Name: 1-Propylpiperazine

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

Identification of 2-aminooxazole amides as acyl-CoA: Diacylglycerol acyltransferase 1 (DGAT1) inhibitors through scaffold hopping strategy was written by Kim, Hyunjin M.;Smith, Michelle D.;Kim, Jae-Hun;Caplen, Mary Ann;Chan, Tin Yau;McKittrick, Brian A.;Cook, John A.;van Heek, Margaret;Lachowicz, Jean. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2013.Safety of tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate This article mentions the following:

A scaffold hopping strategy was successfully applied in discovering 2-aminooxazole amides as potent DGAT1 inhibitors for the treatment of dyslipidemia. Further optimization in potency and PK properties resulted in a lead series with oral in vivo efficacy in a mouse postprandial triglyceridemia (PPTG) assay. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate (cas: 119285-07-3Safety of tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate).

tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate (cas: 119285-07-3) 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. 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.Safety of tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate

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

Small Molecules Targeting the Flavivirus E Protein with Broad-Spectrum Activity and Antiviral Efficacy in Vivo was written by Li, Pi-Chun;Jang, Jaebong;Hsia, Chih-Yun;Groomes, Patrice V.;Lian, Wenlong;de Wispelaere, Melissanne;Pitts, Jared D.;Wang, Jinhua;Kwiatkowski, Nicholas;Gray, Nathanael S.;Yang, Priscilla L.. And the article was included in ACS Infectious Diseases in 2019.Computed Properties of C14H20F3N3 This article mentions the following:

Vaccines and antivirals to combat dengue, Zika, and other flavivirus pathogens present a major, unmet medical need. Vaccine development has been severely challenged by the antigenic diversity of these viruses and the propensity of non-neutralizing, cross-reactive antibodies to facilitate cellular infection and increase disease severity. As an alternative, direct-acting antivirals targeting the flavivirus envelope protein, E, have the potential to act via an analogous mode of action without the risk of antibody-dependent enhancement of infection and disease. We previously discovered that structurally diverse small mol. inhibitors of the dengue virus E protein exhibit varying levels of antiviral activity against other flaviviruses in cell culture. Here, we demonstrate that the broad-spectrum activity of several cyanohydrazones against dengue, Zika, and Japanese encephalitis viruses is due to specific inhibition of E-mediated membrane fusion during viral entry and provide proof of concept for pharmacol. inhibition of E as an antiviral strategy in vivo. 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. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. 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.Computed Properties of C14H20F3N3

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

Nicotinamide Phosphoribosyltransferase Inhibitor as a Novel Payload for Antibody-Drug Conjugates was written by Karpov, Alexei S.;Abrams, Tinya;Clark, Suzanna;Raikar, Ankita;D’Alessio, Joseph A.;Dillon, Michael P.;Gesner, Thomas G.;Jones, Darryl;Lacaud, Marion;Mallet, William;Martyniuk, Piotr;Meredith, Erik;Mohseni, Morvarid;Nieto-Oberhuber, Cristina M.;Palacios, Daniel;Perruccio, Francesca;Piizzi, Grazia;Zurini, Mauro;Bialucha, Carl Uli. And the article was included in ACS Medicinal Chemistry Letters in 2018.Recommanded Product: 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid This article mentions the following:

Antibody-drug conjugates (ADCs) are a novel modality that allows targeted delivery of potent therapeutic agents to the desired site. Herein we report our discovery of NAMPT inhibitors as a novel nonantimitotic payload for ADCs. The resulting anti-c-Kit conjugates (ADC-3 and ADC-4) demonstrated in vivo efficacy in the c-Kit pos. gastrointestinal stromal tumor GIST-T1 xenograft model in a target-dependent manner. In the experiment, the researchers used many compounds, for example, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4Recommanded Product: 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid).

4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4) 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. 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-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid

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

Virtual Screening Approach and Investigation of Structure-Activity Relationships To Discover Novel Bacterial Topoisomerase Inhibitors Targeting Gram-Positive and Gram-Negative Pathogens was written by Magaro, Gabriele;Prati, Federica;Garofalo, Barbara;Corso, Gaia;Furlotti, Guido;Apicella, Claudia;Mangano, Giorgina;D’Atanasio, Noemi;Robinson, Daniel;Di Giorgio, Francesco Paolo;Ombrato, Rosella. And the article was included in Journal of Medicinal Chemistry in 2019.Recommanded Product: tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate This article mentions the following:

Bacterial resistance is increasing rapidly, requiring urgent identification of new antibacterial drugs that are effective against multidrug-resistant pathogens. Novel bacterial topoisomerase inhibitors (NBTIs) provide a new strategy for investigating the well-validated DNA gyrase and topoisomerase IV targets while preventing cross-resistance issues. On this basis, starting from a virtual screening campaign and subsequent structure-based hit optimization guided by X-ray studies, a novel class of piperazine-like NBTIs with outstanding enzymic activity against Staphylococcus aureus and Escherichia coli DNA gyrase and topoisomerase IV was identified. Notably, compounds (±)-33, (±)-35, and (±)-36 with potent and balanced multitarget enzymic profiles exhibited excellent efficacy against selected Gram-pos. and Gram-neg. pathogens, as well as clin. relevant resistant strains. Overall, the new NBTI chemotype described herein, owing to the broad-spectrum antibacterial activity and favorable in vitro safety profile, might serve as a basis for the development of novel treatments against serious infections. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1Recommanded Product: tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate).

tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Recommanded Product: tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate

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

Syntheses of a Triad of Flt3 Kinase Inhibitors: From Bench to Pilot Plant was written by Shieh, Wen-Chung;McKenna, Joe;Sclafani, Joseph A.;Xue, Song;Girgis, Michael;Vivelo, James;Radetich, Branko;Prasad, Kapa. And the article was included in Organic Process Research & Development in 2008.Product Details of 630125-91-6 This article mentions the following:

We have designed and developed an alternative synthesis for the manufacturing of a triad of Flt3 kinase inhibitors (AST487, ATH686, and AUZ454) to support clin. assessments of patients with Flt3-dependent tumor diseases. The new synthesis is convergent, environmentally friendly, practical, and safe and requires no chromatog. purification In the experiment, the researchers used many compounds, for example, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (cas: 630125-91-6Product Details of 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. Product Details of 630125-91-6

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