Category: 630125-91-6

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,630125-91-6

Into a 50-mL round-bottom flask was placed 1-(tert-butoxycarbonyl)-7-((2-methyl-1-(phenylsulfonyl)-1H-pyrrolo[2m3-b]pyridin-4-yl)oxy)-1,2,3,4-tetrahydroquinoline-2-carboxylic acid (300 mg, 0.53 mmol), dichloromethane (20 mL), 4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)aniline (153 mg, 0.53 mmol), N-[(dimethylamino)-1H-1,2,3- triazolo-[4,5-b]pyridin-1-ylmethylene]-N-methylmethanaminium hexafluorophosphate N-oxide (405 mg, 1.06 mmol) and N,N-diisopropylethylamine (0.37 mL, 2.1 mmol). The solution was stirred at 45 C overnight then concentrated. The residue was purified on a silica gel column eluting with ethyl acetate/petroleum ether (1 : 1) to yield tert-Butyl 2-((4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)-7-((2-methyl-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)-3,4-dihydroquinoline-1(2H)-carboxylate (180 mg, 41%).

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

Reference£º
Patent; LYCERA CORPORATION; AICHER, Thomas Daniel; SKALITZKY, Donald J.; TOOGOOD, Peter L.; VANHUIS, Chad A.; (416 pag.)WO2019/200120; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

Into a solution of 4-(4-Ethyl-piperazin-l-ylmethyl)-3-trifluoromethyl- phenylamine (8.0 g, 27.9 mmol, 1.0 eq.) in dichloromethane (140 ml) is added diisopropylethyl amine (5.27 ml, 30.69 mmol, 1.1 eq.). The solution is cooled to O0C, after which 4-Methyl-3- nitrobenzoylchloride (4.18 ml, 28.73 mmol, 1.03 eq.) is added in portions into the reaction EPO mixture which is further equilibrated for 30 minutes. The reaction mixture is then partitioned between dichloromethane and water. The organic layer is separated and the aqueous layer is extracted with dichloromethane. The combined organic extracts are washed with water, dried over Na2SO4, filtered and concentrated to afford the desired product which is used in the next step without further purification.

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£º
Patent; IRM, LLC; WO2006/124462; (2006); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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,630125-91-6

To a solution of 2-chloro-4 6-dimethylpyrimidin-5-amine (50 mg 0.317 mmol) in THF (10 mL) was added triphosgene (33.0 mg 0.111 mmol) . The resulting mixture was stirred at 70 . After LCMS analysis showed the starting material was disappeared. The solvent was removed in vacuo to give 2-chloro-5-isocyanato-4 6-dimethylpyrimidine (50 mg 0.257 mmol 81yield) . To a solution of 4- ( (4-ethylpiperazin-1-yl) methyl) -3- (trifluoromethyl) aniline (94 mg 0.327 mmol) and Et3N (0.114 mL 0.817 mmol) in THF (10 mL) was added a solution of 2-chloro-5-isocyanato-4 6-dimethylpyrimidine (50 mg 0.272 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 dissolved in DCM (60 mL) and washed with H2O (20 mL) and brine (20 mL) . The organic layer was dried over Na2SO4 filtered and concentrated. The residue was purified by preparative HPLC (DCM/MeOH 10/1) to yield a white solid of 1- (2-chloro-4 6-dimethylpyrimidin-5-yl) -3- (4- ( (4-ethylpiperazin-1-yl) methyl) -3- (trifluoromethyl) phenyl) urea (80 mg 0.167 mmol 61.2yield) 1HNMR(400 MHz CD3OD) delta 7.88 (s 1H) 7.39 (d J 8.0 Hz 1H) 6.99 (d J 2.8 Hz 1H) 3.75 (s 2H) 3.04 (m 8H) 2.49 (m 8H) 1.37 (m 3H) ES-LCMS m/z 471.0 (M+H)

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£º
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

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 (17.2 mg, 0.058 mmol) and Na2C03 (37 mg, 0.348 mmol) in DCM (2 ml), kept atooc under argon, 4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine (50 mg, 0.17 4 mmol) was added.The reaction was monitored by HPLC (following the formation of 4-ethyl-piperazine-1-carboxylic acid [4-(4-ethyl-5 piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-amide by treating a sample of the reaction mixture with Nethylpiperazine).After 1 h a solution of 2-[2-amino-5-(3-amino-phenylethynyl)-pyrimidin-4-yl]-1-methyl-1 ,5,6, 7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one (1 04 mg, 0.226 mmol) in DMA (1.5 ml) was added and the reaction was letunder stirring overnight. The mixture was diluted with DCM, washed with water (3 x 10 ml), dried over anhydrousNa2S04 and taken to dryness under vacuum. Purification by flash column chromatography (DCM/MeOH 95/5)10 afforded the product as yellow solid (70 mg, 52%).1H NMR (401 MHz, DMSO-dG) o ppm 0.97 (t, J=7.20 Hz, 3 H) 1.45 (s, 9 H) 2.23- 2.45 (m, 10 H) 3.00 (t, J=6.3 Hz, 2H) 3.51 (s, 2 H) 3.84 (s, 3 H) 4.00 (t, J=6.16 Hz, 2 H) 7.06 (d, J=7.69 Hz, 1 H) 7.11 (s, 2 H) 7.25-7.31 (m, 1 H) 7.43(d, J=8.06 Hz, 1 H) 7.49 (s, 1 H) 7.56- 7.65 (m, 2 H) 7.72 (t, J=1.71 Hz, 1 H) 8.01 (d, J=1.71 Hz, 1 H) 8.50 (s, 1 H),10.00 (bs, 1 H), 10.19 (bs, 1 H).

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£º
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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6,630125-91-6, 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 stirred solution of 4-chloro-3-nitrobenzoic acid (1.0 g, 4.97 mmol) in dichioromethane(10 mL) were added oxalyl chloride (500 jiL, 5.30 mmol) followed by catalytic amount ofDMF and the mixture was stirred at RT for 2 h. The mixture was concentrated under reducedpressure and the residue was dissolved in dichloromethane. The solution was cooled to 0 C;4-((4-ethylpiperazin- 1 -yl)methyl)-3 -(trifluoromethyl)aniline (Intermediate Cl) (1.0 g, 3.30mmol) was added to the reaction mixture followed by DIPEA (1.5 mL, 8.30 mmol). The resultant mixture was stirred overnight at RT. The mixture was diluted with water and extracted twice with ethyl acetate. The combined organic extracts were washed with saturated sodium bicarbonate solution, water and brine. The solution was dried over anhydrous sodiumsulfate, filtered and concentrated. The residue thus obtained was purified by columnchromatography to yield 1.43 g of the desired product. ?H NMR (400 MHz, DMSO-d6) oe0.98 (t, J 7.2 Hz, 3H), 2.28-2.39 (m, 1OH), 3.57 (s, 2H), 7.74 (d, J 8.4 Hz, 1H), 7.98-8.04(m, 2H), 8.16 (s, 1H), 8.27 (dd, J, = 2.4 Hz, J2 = 8.4 Hz, 1H), 8.65 (s, 1H), 10.77 (s, 1H).

The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLENMARK PHARMACEUTICALS S.A.; PATEL, Vinod; REDDY, Venkateshwar; GHARAT, Laxmikant Atmaram; CHAUDHARI, Sachin Sundarlal; DAS, Sanjib; VELGALETI, Ranganadh; SHAH, Daisy Manish; BAJPAI, Malini; (262 pag.)WO2018/215668; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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,630125-91-6

A mixture of starting material (29 mg, 0.1 mmol), 4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline (29 mg, 0.1 mmol), X-Phos (4.3 mg), Pd2(dba)3 (5.5 mg) and K2CO3 (41.5 mg, 0.3 mmol) in t-BuOH (1.5 mL) was heated at 100 C. in a seal tube for 4 h. Then the reaction was filtered through celite and eluted with dichloromethane. The solvent was removed in vacuo and the residue was purified by HPLC to afford the title compound (26.3 mg).

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

Reference£º
Patent; DANA-FARBER CANCER INSTITUTE, INC.; Gray, Nathanael S.; Waller, David; Choi, Hwan Guen; Wang, Jinhua; Deng, Xianming; (104 pag.)US2016/24115; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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

630125-91-6, A mixture of the product of Step C (49 mg, 0.17 mmol) and Intermediate 1(50mg, 0.14 mmol) in 1,4-dioxane (2 mL) was stirred at 100C under N2 for 2 hours (monitored by LCMS).The resulting solution was concentrated under reduced pressure and purified by prep-HPLC to get the title compound (20 mg, 23%) as a white solid. ?H NMR (400 IVIFIz, DMSO-d6) 10.44 (s, 1H), 8.86 (s, 1H), 7.92 (d, J= 5.6 Hz, 1H), 7.90 (d, J= 1.6 Hz, 1H), 7.59 -7.44 (m, 2H), 7.20 (s, 1H), 6.97 – 6.82 (m, 2H), 6.70 (s, 1H), 6.21 (d, J= 5.6 Hz, 1H), 4.95 (d, J= 5.6 Hz, 1H), 3.47 (s, 2H), 2.99 – 2.82 (m, 3H), 2.54 -2.48 (m, 4H), 2.43 – 2.20 (m, 9H), 0.94 (t, J= 7.2 Hz, 3H) ppm.MS: M/e 623 (M+1).

The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BEIGENE, LTD.; ZHOU, Changyou; ZHANG, Guoliang; WO2014/206343; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

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 solution of 100 mg (0.69 mmol) of 3-ethynyl benzoic acid in 5 mL of dry N,N-dimethylformamide, 164 mg (0.57 mmol) of 4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)aniline (prepared as described in J. Med. Chem., (2010) 53, 4701-4719) 242 mg (0.75 mmol) of TBTU and 0.14 mL (0.82 mmol) of DIPEA were added consecutively. After 15 h under stirring at room temperature the mixture was poured into aqueous NaHC03 and extracted twice with ethylacetate. The organic phase was then washed with brine, dried over Na2S04 and evaporated to dryness. A flash- chromatography on silica gel (DCM-MeOH-NH3 7N in methanol 9/1/0.04), afforded 149 mg of the title compound (63%). 1H NMR (600 MHz, DMSO-d6) delta ppm 0.99 (t, J=7.14 Hz, 3 H) 2.19 – 2.46 (m, 10 H) 3.57 (s, 3 H) 6.61 (br. s., 2 H) 7.60 (t, J=7.88 Hz, 1 H) 7.64 (d, J=2.20 Hz, 1 H) 7.72 (d, J=8.61 Hz, 1 H) 7.80 (dt, J=7.83, 1.21 Hz, 1 H) 7.91 – 7.98 (m, 1 H) 8.05 (dd, J=8.52, 1.92 Hz, 1 H) 8.12 (s, 1 H) 8.16 (t, J=1.47 Hz, 1 H) 8.21 (d, J=2.20 Hz, 1 H) 10.59 (s, 1 H) 12.08 (br. s., 1 H) HRMS (ESI) calcd for C29H28N7OF3 [M+H]+ 548.2380, found 548.2392.

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

Reference£º
Patent; NERVIANO MEDICAL SCIENCES S.R.L.; ANGIOLINI, Mauro; BUFFA, Laura; MENICHINCHERI, Maria; MOTTO, Ilaria; POLUCCI, Paolo; TRAQUANDI, Gabriella; ZUCCOTTO, Fabio; WO2014/184069; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics