Category: 314741-40-7

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step F: tert-butyl (3S)-4- F2-(3-cyano-2-fluoro-4-methoxvphenvl)-2-hvdroxvethvll -3- (hydroxymethyl)piperazine- 1 -carboxylateTo a microwave tube containing a stir bar was added 2-fluoro-6-methoxy-3-(oxiran-2- yl)benzonitrile (0.480 g, 2.45 mmol) and tert-butyl (3S)-3-(hydroxymethyl)piperazine-1- carboxylate (1.00 g, 4.92 mmol); the resulting mixture was purged with N2 and the tube washeated in a microwave reactor for 1 h at 150 C. TLC analysis of the reaction mixture showed the completion of the reaction. The solution was concentrated to dryness and absorbed into silica gel and was subjected for purification over a silica column to give title compound

314741-40-7, 314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DEJESUS, Reynalda, Keh; FRIE, Jessica, L.; PIO, Barbara; TANG, Haifeng; WALSH, Shawn, P.; WO2014/99633; (2014); A2;,
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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step F: tert-butyl (3S)-4- F2-(3-cyano-2-fluoro-4-methoxvphenvl)-2-hvdroxvethvll -3- (hydroxymethyl)piperazine- 1 -carboxylateTo a microwave tube containing a stir bar was added 2-fluoro-6-methoxy-3-(oxiran-2- yl)benzonitrile (0.480 g, 2.45 mmol) and tert-butyl (3S)-3-(hydroxymethyl)piperazine-1- carboxylate (1.00 g, 4.92 mmol); the resulting mixture was purged with N2 and the tube washeated in a microwave reactor for 1 h at 150 C. TLC analysis of the reaction mixture showed the completion of the reaction. The solution was concentrated to dryness and absorbed into silica gel and was subjected for purification over a silica column to give title compound

314741-40-7, 314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DEJESUS, Reynalda, Keh; FRIE, Jessica, L.; PIO, Barbara; TANG, Haifeng; WALSH, Shawn, P.; WO2014/99633; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6-Fluoro-2-methyl-3-(oxiran-2-yl)benzonitrile (12.0 g, 67.7 mmol) and (5)-4-N-BOC-2-hydroxymethylpiperazine (22.0 g. 102 mmol) were suspended in ethanol (100 mL) then heated in a microwave apparatus for 30 minutes at 150 C. The reaction mixture was cooled and evaporated dryness. The residue was purified by MPLC chromatography through a 330g Redi-sep column eluting with 5%MeOH/95% EtOAc solvent system to yield the title compound. LC-MS : M+l= 394., 314741-40-7

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PIO, Barbara; PASTERNAK, Alexander; SHAHRIPOUR, Aurash; TANG, Haifeng; WALSH, Shawn; WO2013/90271; (2013); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A solution of iert-butyldimethylsilyl chloride (1.53 g, 10.17 mmol) in DCM (10 ml) was added dropwise to (5)-4-A/-Boc-2-hydroxymethyl-piperazine (2 g, 9.25 mmol) and triethylamine (2.58 ml, 18.49 mmol) in DCM (50 ml) at 20C over a period of 5 minutes under air. The resulting solution was stirred at 20C for 16 hours then evaporated to dryness. The residue was purified by flash silica chromatography, elution gradient 0 to 5% EtOH in EtOAc. Pure fractions were evaporated to dryness to afford te/t-butyl (S)-3-(((ieri-butyldimethylsilyl)oxy)methyl)piperazine-l-carboxylate (2.84 g, 93%) as a colourless oil. 1H NM (500 MHz, CDCI3) 0.00 (s, 6H), 0.84 (s, 9H), 1.40 (s, 9H), 2.48 (s, 1H), 2.6 – 2.87 (m, 3H), 2.92 (d, J = 11.5 Hz, 1H), 3.41 (dd, J = 7.2, 9.8 Hz, 1H), 3.52 (s, 1H), 3.85 (s, 2H).

314741-40-7, The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; BOYD, Scott; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; RAUBO, Piotr, Antoni; (144 pag.)WO2018/206539; (2018); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A solution of iert-butyldimethylsilyl chloride (1.53 g, 10.17 mmol) in DCM (10 ml) was added dropwise to (5)-4-A/-Boc-2-hydroxymethyl-piperazine (2 g, 9.25 mmol) and triethylamine (2.58 ml, 18.49 mmol) in DCM (50 ml) at 20C over a period of 5 minutes under air. The resulting solution was stirred at 20C for 16 hours then evaporated to dryness. The residue was purified by flash silica chromatography, elution gradient 0 to 5% EtOH in EtOAc. Pure fractions were evaporated to dryness to afford te/t-butyl (S)-3-(((ieri-butyldimethylsilyl)oxy)methyl)piperazine-l-carboxylate (2.84 g, 93%) as a colourless oil. 1H NM (500 MHz, CDCI3) 0.00 (s, 6H), 0.84 (s, 9H), 1.40 (s, 9H), 2.48 (s, 1H), 2.6 – 2.87 (m, 3H), 2.92 (d, J = 11.5 Hz, 1H), 3.41 (dd, J = 7.2, 9.8 Hz, 1H), 3.52 (s, 1H), 3.85 (s, 2H).

314741-40-7, The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; BOYD, Scott; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; RAUBO, Piotr, Antoni; (144 pag.)WO2018/206539; (2018); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of the 3-(bromoacetyl)-6-methoxy-2- methylbenzonitrile (2.25 g, 8.40 mmol) in THF was added tert-butyl (35)-3- (hydroxymethyl)piperazine-l -carboxylate (2.18 g, 10.8 mmol) and Hunig’s Base (2.93 mL, 16.8 mmol). The reaction was allowed to stir at RT for 16 hours. TLC showed good reaction at that point. The crude reaction was adsorbed onto silica gel, and purified by silica gel flash chromatography to afford the title compound., 314741-40-7

314741-40-7 (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate 24820294, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PIO, Barbara; PASTERNAK, Alexander; SHAHRIPOUR, Aurash; TANG, Haifeng; WALSH, Shawn; WO2013/90271; (2013); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

1-fluoro-4-nitrobenzene (1.460 g, 10.4 mmol) and potassium carbonate (4.29 g, 31.0 mmol) were suspended inanhydrous DMF (10 mL) . (S)-tert-butyl 3- (hydroxymethyl)piperazine-1-carboxylate (2.35 g, 10.9 mmol) was added and the mixture was heated at 90 C for 21 h. After cooling the mixture was partitioned between brine/water (100 mL) and ethyl acetate (25 mL) . Theaqueous layer was separated and further extracted with ethyl acetate (3 x 25 mL) . The combined ethyl acetate fractions were washed with brine/water (1:1, 4 x 25 mL), dried (anhydrous sodium sulfate), filtered and reduced in vacuo. The resulting residue was purified by silica gelchromatography (gradient 25-100% ethyl acetate incyclohexane) to afford the title compound (0.99 g, 28.4%) . ?H NMR (400 MHz, CDC13) : 3 8.12 (d, 2H), 6.83 (d, 2H),4.20-4.46 (m, 1H), 4.02-4.14 (m, 2H), 3.48-3.76 (m, 3H),3.08-3.30 (m, 3H), 2.86 (br s, 1H), 1.50 (s, 9H) . LCMS(Method C) : = 1.38 mi m/z = 338 [M+H]., 314741-40-7

As the paragraph descriping shows that 314741-40-7 is playing an increasingly important role.

Reference：
Patent; ALMAC DISCOVERY LIMITED; HARRISON, Timothy; TREVITT, Graham; HEWITT, Peter Robin; O’DOWD, Colin Roderick; BURKAMP, Frank; WILKINSON, Andrew John; SHEPHERD, Steven D.; MIEL, Hugues; WO2015/92431; (2015); 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Compound 2Sa (3.0 g, 18.8 mmol), compound 2Sb (3.0 g, 13.8 mmol, 100% ee) and potassium hydroxide (2.4 g, 42.8 mmol) were added sequentially to 30 mL DMSO while stirring. The reaction mixture was heated to 30C. for 3 hours and then warmed to 60C. for 5 hours. After completion of the reaction, the system was cooled to room temperature, 300 mL of water was added, precipitation formed, and stirring was continued at room temperature overnight. Solid was collected via filtering, and and was added to 25 mL of a mixed solvent consisting of 5:1 petroleum ether:ethyl acetate, and stirred at room temperature for half an hour. The solid was collected via filtering, and was dried to give compound 2Sc (3.0 g, yield 64%) as a yellow solid. MS 336.2 [M+H]+.

314741-40-7, As the paragraph descriping shows that 314741-40-7 is playing an increasingly important role.

Reference：
Patent; Hangzhou Innogate Pharma Co., Ltd.; ZHANG, Hancheng; LIU, Shifeng; (40 pag.)US2019/100531; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

314741-40-7, (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2,6-difluoro-3-(oxiran-2-yl)benzonitrile (1.50 g, 8.28 mmol) and (S)-4-N-BOC-2-hydroxymethylpiperazine (2.40g, 11.1 mmol) were suspended in ethanol (15 mL) then heated in a microwave apparatus for 30 min at 150 C. Thereaction mixture was cooled and evaporated dryness. The residue was purified by chromatography through a 120gRedi-sep column eluting with 5%MeOH/95% EtOAc to yield the title compound LC-MS: M+1 = 398

314741-40-7, The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Merck Sharp & Dohme Corp.; PASTERNAK, Alexander; BLIZZARD, Timothy; CHOBANIAN, Harry; DE JESUS, Reynalda; DING, Fa-Xiang; DONG, Shuzhi; GUDE, Candido; KIM, Dooseop; TANG, Haifeng; WALSH, Shawn; PIO, Barbara; JIANG, Jinlong; (128 pag.)EP2744499; (2016); B1;,
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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Step C: tert-butyl (38)-4-[2-(2, 1 ,3-benzoxadiazol-5-yl)-2-hydroxyethyll -3-(hydroxymethyl)piperazine-1-carboxylate: To a microwave tube containing a stir bar was added5-(oxiran-2-yl)-2,1,3-benzoxadiazole (1.2 g, 7.4 mmol), Boc-piperizine alcohol (2.8 g, 13.3mmol); the resulting mixture was dissolved in anhydrous toluene (15 mL), purged with N2 andthe tube was heated in a microwave reactor for 1 h at 150 C. TLC analysis of the rectrion mix.showed the completion of the reaction. The solution was concentrated to dryness and absorbed into silica gel and was subjected for purification over a silica column to give the title compound., 314741-40-7

The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DEJESUS, Reynalda, Keh; FRIE, Jessica, L.; PIO, Barbara; TANG, Haifeng; WALSH, Shawn, P.; WO2014/99633; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics