Category: 1188265-73-7

1188265-73-7, tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

DIPEA (5.24 ml, 30.06 mmol) was added to a stirred mixture of ferf-butyl 3-(2-hydroxyethyl)piperazine-l-carboxylate (1.73 g, 7.51 mmol) and 7-bromo-4-chloro-5,8-difluoroquinazoline (2.1 g, 7.51 mmol) in MeCN (100 ml) at room temperature. The resulting solution was stirred at room temperature for 3 hours, a suspension developed after ~30 minutes. The precipitate was collected by filtration, washed with MeCN (3 x 20 ml) and dried under vacuum to afford desired product, 2.64 g. On standing overnight a second crop of desired product, 300 mgs was isolated to afford ferf-butyl 4-(7-bromo-5,8-difluoroquinazolin-4-yl)-3-(2-hydroxyethyl)piperazine-l-carboxylate (2.94 g, 83%), as a white solid, which was used without further purification. 1H NM R (400 MHz, DMSO, 30C) 1.43 (9H, s), 1.71 – 1.82 (2H, m), 2.86 (1H, s), 3.18 (1H, s), 3.37 – 3.51 (2H, m), 3.72 (1H, d), 3.97 (2H, d), 4.36 (1H, s), 4.70 (1H, s), 7.75 (1H, dd), 8.62 (1H, s) OH not observed, m/z (ES+), [M+H]+ 473, 475., 1188265-73-7

As the paragraph descriping shows that 1188265-73-7 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; LAMONT, Scott, Gibson; KEMMITT, Paul, David; GOLDBERG, Frederick, Woolf; (158 pag.)WO2019/215203; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1188265-73-7, tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

DIPEA (5.24 ml, 30.06 mmol) was added to a stirred mixture of ferf-butyl 3-(2-hydroxyethyl)piperazine-l-carboxylate (1.73 g, 7.51 mmol) and 7-bromo-4-chloro-5,8-difluoroquinazoline (2.1 g, 7.51 mmol) in MeCN (100 ml) at room temperature. The resulting solution was stirred at room temperature for 3 hours, a suspension developed after ~30 minutes. The precipitate was collected by filtration, washed with MeCN (3 x 20 ml) and dried under vacuum to afford desired product, 2.64 g. On standing overnight a second crop of desired product, 300 mgs was isolated to afford ferf-butyl 4-(7-bromo-5,8-difluoroquinazolin-4-yl)-3-(2-hydroxyethyl)piperazine-l-carboxylate (2.94 g, 83%), as a white solid, which was used without further purification. 1H NM R (400 MHz, DMSO, 30C) 1.43 (9H, s), 1.71 – 1.82 (2H, m), 2.86 (1H, s), 3.18 (1H, s), 3.37 – 3.51 (2H, m), 3.72 (1H, d), 3.97 (2H, d), 4.36 (1H, s), 4.70 (1H, s), 7.75 (1H, dd), 8.62 (1H, s) OH not observed, m/z (ES+), [M+H]+ 473, 475., 1188265-73-7

As the paragraph descriping shows that 1188265-73-7 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; LAMONT, Scott, Gibson; KEMMITT, Paul, David; GOLDBERG, Frederick, Woolf; (158 pag.)WO2019/215203; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1188265-73-7, tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

DIPEA (5.24 ml, 30.06 mmol) was added to a stirred mixture of ferf-butyl 3-(2-hydroxyethyl)piperazine-l-carboxylate (1.73 g, 7.51 mmol) and 7-bromo-4-chloro-5,8-difluoroquinazoline (2.1 g, 7.51 mmol) in MeCN (100 ml) at room temperature. The resulting solution was stirred at room temperature for 3 hours, a suspension developed after ~30 minutes. The precipitate was collected by filtration, washed with MeCN (3 x 20 ml) and dried under vacuum to afford desired product, 2.64 g. On standing overnight a second crop of desired product, 300 mgs was isolated to afford ferf-butyl 4-(7-bromo-5,8-difluoroquinazolin-4-yl)-3-(2-hydroxyethyl)piperazine-l-carboxylate (2.94 g, 83%), as a white solid, which was used without further purification. 1H NM R (400 MHz, DMSO, 30C) 1.43 (9H, s), 1.71 – 1.82 (2H, m), 2.86 (1H, s), 3.18 (1H, s), 3.37 – 3.51 (2H, m), 3.72 (1H, d), 3.97 (2H, d), 4.36 (1H, s), 4.70 (1H, s), 7.75 (1H, dd), 8.62 (1H, s) OH not observed, m/z (ES+), [M+H]+ 473, 475., 1188265-73-7

As the paragraph descriping shows that 1188265-73-7 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; LAMONT, Scott, Gibson; KEMMITT, Paul, David; GOLDBERG, Frederick, Woolf; (158 pag.)WO2019/215203; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1188265-73-7, tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1188265-73-7, Intermediate 11 2-[1-(5-Aminothiazolo[5,4-d]pyrimidin-7-yl)piperazin-2-yl]ethanol trifluoracetate salt [0231] To a solution of Intermediate 4 (0.38 g, 2.06 mmol) in DMF (20 mL) were added tert-butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate (1 g, 4.12 mmol) and DIPEA (0.4 g, 3.0 mmol). The reaction mixture was heated at 100 C. for 5 h, allowed to cool, then stirred at room temperature for 2 days. The reaction mixture was concentrated in vacuo, then partitioned between water and DCM. The organic phase was separated and concentrated in vacuo. The resulting crude material was purified by column chromatography (silica gel: 100-200 mesh, MeOH:DCM gradient 0% to 20%) to give a pale yellow foam. The foam was dissolved in DCM (1 mL) and TFA (2 mL) and stirred for 1 h. The reaction mixture was concentrated in vacuo, then triturated with diethyl ether, to give the title compound (0.6 g) as a sticky yellow solid. LCMS (ES+) 281 (M+H)+, RT 0.361 minutes (method 3).

1188265-73-7 tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate 53407692, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Brookings, Daniel Christopher; Ford, Daniel James; Franklin, Richard Jeremy; Ghawalkar, Anant Ramrao; Kulisa, Claire Louise; Neuss, Judi Charlotte; Reuberson, James Thomas; US2014/315885; (2014); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1188265-73-7, tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

fert-Butyl 3 -(2-hydroxy ethyl) piperazine-1 -carboxylate(6.91 g, 30.0 mmol) and 5-(2-bromoacetyl)-4-methylisobenzofuran-l(3H)-one (6.73 g, 25 mmol) were dissolved in tetrahydrofuran (100 mL) then added Hunig’s base (8.73 mL, 50.0 mmol) and stirred at RT overnight. The reaction was poured into brine and extracted with EtOAc (2x). The combined organic layer was dried over Na2SC”4, filtered and evaporated to dryness. The crude product was chromatographed through an ISCO Redi-Sep 330g column and eluted with 5% MeOH /DCM solvent system to the title compound. LC-MS (IE, m/z): 419 [M + 1]+ ., 1188265-73-7

The synthetic route of 1188265-73-7 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

1188265-73-7, tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step B: tert – butyl 3-(2-hydroxyethvn-4-(2-(4-methyl-l-oxo-l,3-dihvdroisobenzofuran-5-yl-2-oxoethyPpiperazine- 1 -carboxylate : tert-Butyl 3-(2-hydroxyethyl) piperazine-1 -carboxylate (6.91 g, 30.0 mmol) and 5-(2-bromoacetyl)-4-methylisobenzofuran-l(3H)-one (6.73 g, 25 mmol) were dissolved in tetrahydrofuran (100 mL) then added Hunig’s base (8.73 mL, 50.0 mmol) and stirred at RT overnight. The reaction was poured into brine and extracted with EtOAc (2x). The combined organic layer was dried over Na2S04, filtered and evaporated to dryness. The crude product was chromatographed through an ISCO Redi-Sep 330g column and eluted with 5% MeOH /DCM solvent system to the title compound. LC-MS (IE, m/z): 419 [M + 1]+ ., 1188265-73-7

As the paragraph descriping shows that 1188265-73-7 is playing an increasingly important role.

Reference£º
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; WO2013/28474; (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.1188265-73-7,tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

Phenyl (4-chloro-3-fluorophenyl)carbamate (441 mg, 1.659 mmol) and tert-butyl 3-(2- hydroxyethyl)piperazine-l-carboxylate (382 mg, 1.659 mmol) were suspended in EtOH (5 niL) and heated in a Biotage Initiator using initial high setting to 100 C for 7 min. The reaction was concentrated under a stream of nitrogen at 50 C then dissolved in DCM (3 niL) and TFA (3 niL, 38.9 mmol). After 30 minutes the reaction was concentrated under a stream of nitrogen at 50 C. The residue was dissolved in DCM/MeOH and loaded onto a SCX-3 cartridge (2 g). The cartridge was washed with 3 volumes of MeOH, then eluted with 3 volumes of 2N NH3MeOH. The eluants were concentrated under a stream of nitrogen at 50 C followed by high vacuum, resulting in the isolation of N-(4-chloro-3-fluorophenyl)-2-(2 -hydro xyethyl)piperazine-l-carboxamide (494 mg, 1.637 mmol, 99 % yield) as a white solid.LC/MS (ESI): m/z 302.0 (M+H)+, 0.39 min (ret. time)

1188265-73-7, 1188265-73-7 tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate 53407692, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; BAILEY, James; CHEN, Yao; HURLE, Mark; LEACH, Craig; TURUNEN, Brandon; (103 pag.)WO2018/134731; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1188265-73-7, tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

DIPEA (5.24 ml, 30.06 mmol) was added to a stirred mixture of ferf-butyl 3-(2-hydroxyethyl)piperazine-l-carboxylate (1.73 g, 7.51 mmol) and 7-bromo-4-chloro-5,8-difluoroquinazoline (2.1 g, 7.51 mmol) in MeCN (100 ml) at room temperature. The resulting solution was stirred at room temperature for 3 hours, a suspension developed after ~30 minutes. The precipitate was collected by filtration, washed with MeCN (3 x 20 ml) and dried under vacuum to afford desired product, 2.64 g. On standing overnight a second crop of desired product, 300 mgs was isolated to afford ferf-butyl 4-(7-bromo-5,8-difluoroquinazolin-4-yl)-3-(2-hydroxyethyl)piperazine-l-carboxylate (2.94 g, 83%), as a white solid, which was used without further purification. 1H NM R (400 MHz, DMSO, 30C) 1.43 (9H, s), 1.71 – 1.82 (2H, m), 2.86 (1H, s), 3.18 (1H, s), 3.37 – 3.51 (2H, m), 3.72 (1H, d), 3.97 (2H, d), 4.36 (1H, s), 4.70 (1H, s), 7.75 (1H, dd), 8.62 (1H, s) OH not observed, m/z (ES+), [M+H]+ 473, 475., 1188265-73-7

As the paragraph descriping shows that 1188265-73-7 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; LAMONT, Scott, Gibson; KEMMITT, Paul, David; GOLDBERG, Frederick, Woolf; (158 pag.)WO2019/215203; (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.1188265-73-7,tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,1188265-73-7

Step 2: 3-(2-Hydroxy-ethyl)-piperazine-1-carboxylic acid tert-butyl ester (58 mg, 0.25 mmol) was dissolved in 4 mL of dichloromethane and 1 mL of DIPEA, and then triphosgene (27 mg, 0.09 mmol) was added at room temperature. The reaction mixture was stirred for 30 minutes, and the solvent was removed in vacuo. The residue was dissolved in 3 mL of dichloromethane and 1 mL of TFA. After the reaction mixture was stirred for 1 hour, the solvent was removed in vacuo to give hexahydro-pyrazino[1,2-c][1,3]oxazin-6-one trifluoro acetitic acid salt (Compound D) as a crude product which was used directly without further purification. LC/MS: calc’d 157 (MH+), exp 157 (MH+).

As the paragraph descriping shows that 1188265-73-7 is playing an increasingly important role.

Reference£º
Patent; HOFFMANN-LA ROCHE INC.; Guo, Lei; Hu, Taishan; Kou, Buyu; Lin, Xianfeng; Shen, Hong; Shi, Houguang; Yan, Shixiang; Zhang, Weixing; Zhang, Zhisen; Zhou, Mingwei; Zhu, Wei; US2015/252057; (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.1188265-73-7,tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

tert-butyl 3-(2-hydroxyethyl) piperazine-1-carboxylate (6.91 g, 30.0 mmol) and 5-(2-bromoacetyl)-4-methylisobenzofuran-1(3H)-one (6.73 g, 25 mmol) were dissolved in tetrahydrofuran (100 mL) then added Hunig?sbase (8.73 mL, 50.0 mmol) and stirred at RT overnight. The reaction was poured into brine and extracted with EtOAc(2x). The combined organic layer was dried over Na2SO4, filtered and evaporated to dryness. The crude productwas chromatographed through an ISCO Redi-Sep 330g column and eluted with 5% MeOH /DCM solvent systemto the title compound. LC-MS (IE, m/z): 419 [M + 1]+., 1188265-73-7

1188265-73-7 tert-Butyl 3-(2-hydroxyethyl)piperazine-1-carboxylate 53407692, apiperazines compound, is more and more widely used in various fields.

Reference£º
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