Category: 129799-15-1

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,129799-15-1

To a solution of 1-tert-butyl 2-methyl piperazine-1, 2-dicarboxylate (0.2g, 0.82 mmol) and triethylamine (1.2 mL, 8.2 mmol) in anhydrous THF (5 mL) atrt was added trimethylsilyl isocyanate (1.1 mL, 8.2 mmol) dropwise. The mixturewas stirred at rt for 8 h and quenched with ice-water (10 mL) , and then THFwas removed. The aqueous layer was extracted with EtOAc (10 mL × 3) . The combined organiclayers were dried over anhydrous Na2SO4 and concentratedto give 1-tert-butyl 2-methyl 4-carbamoylpiperazine-1, 2-dicarboxylate asa white solid (0.3 g, 90) . 1H NMR (400 MHz, CDCl3): delta ppm 4.24 (br.s, 2H) , 4.30 (d, J 13.3 Hz, 1H) , 3.98-4.14 (m, 1H) ,3.83-3.94 (m, 1H) , 3.78 (s, 3H) , 3.18-3.28 (m, 1H) , 3.03-3.12 (m, 1H) ,2.79-2.96 (m, 1H) , 1.50 (d, J 16.7 Hz, 9H) and MS-ESI: m/z 232.25 [M-55] +.

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,129799-15-1

To a solution of 1-tert-butyl 2-methyl piperazine-1, 2-dicarboxylate (0.2g, 0.82 mmol) and triethylamine (1.2 mL, 8.2 mmol) in anhydrous THF (5 mL) atrt was added trimethylsilyl isocyanate (1.1 mL, 8.2 mmol) dropwise. The mixturewas stirred at rt for 8 h and quenched with ice-water (10 mL) , and then THFwas removed. The aqueous layer was extracted with EtOAc (10 mL × 3) . The combined organiclayers were dried over anhydrous Na2SO4 and concentratedto give 1-tert-butyl 2-methyl 4-carbamoylpiperazine-1, 2-dicarboxylate asa white solid (0.3 g, 90) . 1H NMR (400 MHz, CDCl3): delta ppm 4.24 (br.s, 2H) , 4.30 (d, J 13.3 Hz, 1H) , 3.98-4.14 (m, 1H) ,3.83-3.94 (m, 1H) , 3.78 (s, 3H) , 3.18-3.28 (m, 1H) , 3.03-3.12 (m, 1H) ,2.79-2.96 (m, 1H) , 1.50 (d, J 16.7 Hz, 9H) and MS-ESI: m/z 232.25 [M-55] +.

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (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.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

The compound (S) -5- (1 – ((tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4-(difluoromethoxy) phenyl ) -oxazole-4-carboxylic Acid (0.25g, 0.53mmol), 1-Boc-2- piperazine carboxylate(157mg, 0.64mmol), 1- ethyl-3- (3-dimethylaminopropyl) carbodiimide Hydrochloride (153mg, 0.80mmol)and N- hydroxy-7-aza-benzotriazole (181mg, 1.33mmol) was dissolved in dichloromethane (20mL) Theconditions at 0 C to this solution was added dropwise N, N- diisopropylethylamine (0.37mL, 2.13mmol), 5Hstirred at room temperature, the solvent was removed, Concentrate was separated by column chromatography(eluent: Petroleumether / EtOAc (v / v) = 3/1), to give 260mg colorless viscous substance, yield: 70.

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Guangdong East Sunshine Pharmaceutical Co., Ltd; Zhang, Ying jun; Liu, Bing; Yu, Tian Zhu; Zhang, Xiang Yu; (348 pag.)CN105399698; (2016); A;,
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.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

Example 111a 1-tert-Butyl 2-Methyl 4-benzylpiperazine-1,2-dicarboxylate 111a To a dry 100 ml one necked round bottom flask equipped with a stirring bar was added 1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (5 g, 20.5 mmol) under N2 (). Anhydrous acetonitrile (60 mL) was added followed by the additions of BnBr (2.7 mL, 22.5 mmol) and triethylamine (8.5 ml, 61.5 mmol). A condenser was then put on to the flask and the reaction mixture was heated at 71 C. for 45 minutes. The reaction mixture was allowed to come to room temperature and concentrated under reduced pressure. It was then diluted with dichloromethane and washed with water and brine. The organic layer was dried over Na2SO4, filtered and concentrated under reduced pressure. The crude compound was purified with flash column (PE: EA=8:1) to yield 4.5 g (66%) of 111a. MS: [M+H]+: 335, 129799-15-1

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GENENTECH, INC.; Crawford, James John; Young, Wendy B.; US2013/116245; (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.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

Example 111a 1-tert-Butyl 2-Methyl 4-benzylpiperazine-1,2-dicarboxylate 111a To a dry 100 ml one necked round bottom flask equipped with a stirring bar was added 1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (5 g, 20.5 mmol) under N2 (). Anhydrous acetonitrile (60 mL) was added followed by the additions of BnBr (2.7 mL, 22.5 mmol) and triethylamine (8.5 ml, 61.5 mmol). A condenser was then put on to the flask and the reaction mixture was heated at 71 C. for 45 minutes. The reaction mixture was allowed to come to room temperature and concentrated under reduced pressure. It was then diluted with dichloromethane and washed with water and brine. The organic layer was dried over Na2SO4, filtered and concentrated under reduced pressure. The crude compound was purified with flash column (PE: EA=8:1) to yield 4.5 g (66%) of 111a. MS: [M+H]+: 335, 129799-15-1

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GENENTECH, INC.; Crawford, James John; Young, Wendy B.; US2013/116245; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A 25 mL rb flask equipped with a rubber septum and a magnetic stir bar was set under an Ar atmosphere and charged with 840 mg of l-/er/-butyl 2-methyl piperazine- l,2-dicarboxylate 42 (3.44 mmol, 1 equiv.) dissolved in 6.9 mL of CH2CI2. After the reaction mixture was cooled to 0 C, 0.527 mL of TEA (3.78 mmol, 1.1 equiv.) and 0.515 mL of CbzCl (3.61 mmol, 1.05 equiv.) were added dropwise and the reaction mixture was stirred for 30 min. Then the reaction mixture was allowed to warm to rt and stirring was continued for 2 h. The reaction mixture was quenched by addition of sat. NLLCl solution, extracted with CH2CI2 (2x), washed with sat. NaHCCh solution (2x), brine and dried over Na2S04. The crude product was purified on silica gel column using 30 % EA in hexanes as eluent affording 986 mg (76 %) of the product 42 as a colorless oil., 129799-15-1

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; EMORY UNIVERSITY; LIOTTA, Dennis C.; JECS, Edgars; ALTAS TAHIROVIC, Yesim; WILSON, Lawrence; PELLY, Stephen Christopher; (102 pag.)WO2019/183133; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a mixture of 1-tert-butyl 2-methyl piperazine- 1,2-dicarboxylate (5.0 g, 22.6 mmol, 1.00 eq) in MeOH (50.0 mL) was added HCl/dioxane (4.0 M, 134 mL). The reaction mixture was degassed and purged with nitrogen 3 times, and the mixture was stirred at 25 C for 12 hours under a nitrogen atmosphere. The reaction mixture was concentrated under reduced pressure to dryness to give methyl piperazine- 2-carboxylate (4.89 g, 2HC1, crude) as a white solid, which was used directly in the next step without further purification.

129799-15-1, 129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; MIRATI THERAPEUTICS, INC.; ARRAY BIOPHARMA, INC.; FISCHER, John, P.; FELL, Jay, Bradford; BLAKE, James, F.; HINKLIN, Ronald, Jay; MEJIA, Macedonio, J.; HICKEN, Erik, James; CHICARELLI, Mark, Joseph; GAUDINO, John, J.; VIGERS, Guy, P.A.; BURGESS, Laurence, E.; MARX, Matthew, Arnold; CHRISTENSEN, James, Gail; LEE, Matthew, Randolf; SAVECHENKOV, Pavel; ZECCA, Henry, J.; (529 pag.)WO2017/201161; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

129799-15-1, EXAMPLE 20 Preparation of 1-tert-butyl 2-methyl 4-(4-chlorophthalazin-1-yl)piperazine-1,2-dicarboxylate (JK-16) 1,4-dichlorophthalazine (741 mg, 3.72 mmol), 1-tert-butyl 2-methyl piperazine-1,2-dicarboxylate (1.00 g, 4.09 mmol), N,N-diisopropylethylamine (0.972 mL), and 4-methyl-2-pentanone (6 mL) were heated at 120 for 16 hours. The solvent was removed and the residue purified by chromatography over silica using a gradient of hexanes/0-70% ethyl acetate. The compound was obtained as a white solid. MS (M+H)+=407.1.

129799-15-1 Methyl 1-Boc-piperazine-2-carboxylate 2756818, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Amgen Inc.; US2009/48259; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

129799-15-1, Methyl 1-Boc-piperazine-2-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of methyl 1-Boc-piperazine-2-carboxylate (0.5 g, 2 mmol) in CH2Cl2 (10 ml) was added PhSO2Cl (0.53 ml,4.1 mmol) and Et3N (0.57 ml, 4.1 mmol) at room temperature. The resulting solution was stirred overnight. The reaction was washed with 1 N NaHCO3 (40mL x 3), brine and dried over Na2SO4. The product was purified via flash chromatography (10% EtOAc/Hexanes; 20% EtOAc/Hexanes; 50% EtOAc/Hexanes) to give an off-white solid Methyl 1-Boc-4-benzenesulfonyl-piperazine-2-carboxylate in 91% yield., 129799-15-1

The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Zhao, Huanyu; Prosser, Anthony R.; Liotta, Dennis C.; Wilson, Lawrence J.; Bioorganic and Medicinal Chemistry Letters; vol. 25; 21; (2015); p. 4950 – 4955;,
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.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.

Step 6 Synthesis of 4-(5-Fluoro-2-trifluoromethyl-benzoyl)-piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester DIPEA (430 mg, 0.58 mL, 3.27 mmol) followed by HOBT (121 mg, 0.9 mmol) and EDCI (230 mg, 1.22 mmol) were added to a stirred solution of 5-Fluoro-2-trifluoromethyl-benzoic acid (170 mg, 0.82 mmol) in DMF (2.0 mL) at room temperature. After 2 minutes 2 minutes piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester (200 mg, 0.82 mmol) was added and the resulting mixture was stirred at room temperature overnight. Cold water was then added, filtered the solid precipitated to afford 305 mg (85.9%) of 4-(5-Fluoro-2-trifluoromethyl-benzoyl)-piperazine-1,2-dicarboxylic acid 1-tert-butyl ester 2-methyl ester.

129799-15-1, As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.

Reference：
Patent; Bischoff, Alexander; Subramanya, Hosahalli; Sundaresan, Kumar; Sammeta, Srinivasa Raju; Vaka, Anil Kumar; US2010/160323; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics