Category: 163765-44-4

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl (3R)-3-methylpiperazine-1-carboxylate (500 mg, 2.5mmol), 6-chloropyridine-3-carbonitrile (415 mg, 3 mmol) in DMSO (10 mL), potassiumcarbonate (690 mg, 5 mmol), Cu (MeCN)4PF6(18 mg, 0.05 mmol) were added at RT. Thereaction mixture was heated at 140 C for 4 h (TLC indicated complete consumption of thestarting materials), brought toRT, diluted with water (30 mL) and extracted with EtOAc (3 x40 mL). The combined organic extracts were washed with water (30 mL), brine (40 mL),dried over Na2S04 and concentrated under reduced pressure to afford the crude compound.The crude material was purified by column chromatography (100-200 mesh silica gel, 7 g,30% EtOAc-hexane) to afford tert-butyl (3R)-4-(5-cyano-2-pyridyl)-3-methyl-piperazine-1-carboxylate (415 mg, 55%) as an off-white solid.1H NMR [300 MHz, CDCh]: J 8.39 (d, J = 2.4 Hz, 1H), 7.62-7.58 (m, 1H), 6.54 (d, J = 9.0Hz, 1H), 4.51 (brs, 1H), 4.13-3.89 (m, 3H), 3.27-3.13 (m, 2H), 3.00 (brs, 1H), 1.45 (s, 9H),1.23-1.16 (m, 3H).LCMS: m/z: 247.46 [M-tBu] +., 163765-44-4

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; MITOBRIDGE, INC.; TAKAHASHI, Taisuke; KLUGE, Arthur; LAGU, Bharat; JI, Nan; (162 pag.)WO2018/125961; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

163765-44-4, The compound (R) -3- methyl-piperazine-1-carboxylate (250mg, 1.25mmol), cyclopropanecarboxylic acid(130mg, 1.50mmol), 1- Ethyl-3- (3-dimethylaminopropyl) carbodiimide hydrochloride (480mg, 2.50mmol)and N- hydroxy-7-aza-benzotriazole (254mg, 1.87 mmol) were dissolved in dichloromethane (10 mL), and theconditions under 0 C, to this solution was added dropwise N, N- diisopropylethylamine (0.65mL, 3.74mmol), stirred for 10H at room temperature, add water (10mL × 3) washing the organic phase was dried overanhydrous Na 2 SO 4, the solvent was removed, the concentrate was subjected to column Chromatography(eluent: Petroleumether / EtOAc (v / v) = 2/1), to give 310mg of colorless liquid: (R) -4- (cyclopropylcarbonyl)-3- Methyl-piperazine-1-carboxylate, yield: 93%.

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

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

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

163765-44-4, The compound (R) -3- methyl-piperazine-1-carboxylate (250mg, 1.25mmol), cyclopropanecarboxylic acid(130mg, 1.50mmol), 1- Ethyl-3- (3-dimethylaminopropyl) carbodiimide hydrochloride (480mg, 2.50mmol)and N- hydroxy-7-aza-benzotriazole (254mg, 1.87 mmol) were dissolved in dichloromethane (10 mL), and theconditions under 0 C, to this solution was added dropwise N, N- diisopropylethylamine (0.65mL, 3.74mmol), stirred for 10H at room temperature, add water (10mL × 3) washing the organic phase was dried overanhydrous Na 2 SO 4, the solvent was removed, the concentrate was subjected to column Chromatography(eluent: Petroleumether / EtOAc (v / v) = 2/1), to give 310mg of colorless liquid: (R) -4- (cyclopropylcarbonyl)-3- Methyl-piperazine-1-carboxylate, yield: 93%.

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

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

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (R) -tert-butyl 3-methylpiperazine-1-carboxylate (200 mg, 1.00mmol) , 2-cyclopropylacetic acid (120 mg, 1.20 mmol) , EDCI (287mg, 1.50 mmol) and HOAT (340 mg, 2.50 mmol) in DCM (20 mL) was stirred at 0 , and DIPEA (0.70 mL, 4.00mmol) was added dropwise. After the addition, the mixture was stirred at rt for16 h and washed with water (10 mL × 2) . The organiclayer was dried over anhydrous Na2SO4 and concentrated.The residue was purified by silica gel chromatography eluted with Petroleumether/EtOAc (v/v) 2/1 to give (R) -tert-butyl 4-(2-cyclopropylacetyl) -3-methylpiperazine-1-carboxylate as colorless oil (260mg, 92) . 1H NMR (400 MHz, CDCl3): delta ppm 3.85-4.14 (m, 3H) , 3.31-3.55 (m, 1H) , 2.80-2.97 (m, 3H) , 2.30-2.33,2.20-2.23 (m, m, 0.5H, 1.5H) , 1.46 (s, 9H) , 1.15-1.24 (m, 3H) , 1.03-1.07 (m,1H) , 0.55-0.57 (m, 2H) , 0.15-0.18 (m, 2H) ., 163765-44-4

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

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

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (R) -tert-butyl 3-methylpiperazine-1-carboxylate (200 mg, 1.00mmol) , 2-cyclopropylacetic acid (120 mg, 1.20 mmol) , EDCI (287mg, 1.50 mmol) and HOAT (340 mg, 2.50 mmol) in DCM (20 mL) was stirred at 0 , and DIPEA (0.70 mL, 4.00mmol) was added dropwise. After the addition, the mixture was stirred at rt for16 h and washed with water (10 mL × 2) . The organiclayer was dried over anhydrous Na2SO4 and concentrated.The residue was purified by silica gel chromatography eluted with Petroleumether/EtOAc (v/v) 2/1 to give (R) -tert-butyl 4-(2-cyclopropylacetyl) -3-methylpiperazine-1-carboxylate as colorless oil (260mg, 92) . 1H NMR (400 MHz, CDCl3): delta ppm 3.85-4.14 (m, 3H) , 3.31-3.55 (m, 1H) , 2.80-2.97 (m, 3H) , 2.30-2.33,2.20-2.23 (m, m, 0.5H, 1.5H) , 1.46 (s, 9H) , 1.15-1.24 (m, 3H) , 1.03-1.07 (m,1H) , 0.55-0.57 (m, 2H) , 0.15-0.18 (m, 2H) ., 163765-44-4

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

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

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (R) -tert-butyl 3-methylpiperazine-1-carboxylate (200 mg, 1.00mmol) , 2-cyclopropylacetic acid (120 mg, 1.20 mmol) , EDCI (287mg, 1.50 mmol) and HOAT (340 mg, 2.50 mmol) in DCM (20 mL) was stirred at 0 , and DIPEA (0.70 mL, 4.00mmol) was added dropwise. After the addition, the mixture was stirred at rt for16 h and washed with water (10 mL × 2) . The organiclayer was dried over anhydrous Na2SO4 and concentrated.The residue was purified by silica gel chromatography eluted with Petroleumether/EtOAc (v/v) 2/1 to give (R) -tert-butyl 4-(2-cyclopropylacetyl) -3-methylpiperazine-1-carboxylate as colorless oil (260mg, 92) . 1H NMR (400 MHz, CDCl3): delta ppm 3.85-4.14 (m, 3H) , 3.31-3.55 (m, 1H) , 2.80-2.97 (m, 3H) , 2.30-2.33,2.20-2.23 (m, m, 0.5H, 1.5H) , 1.46 (s, 9H) , 1.15-1.24 (m, 3H) , 1.03-1.07 (m,1H) , 0.55-0.57 (m, 2H) , 0.15-0.18 (m, 2H) ., 163765-44-4

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

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

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of (R) -tert-butyl 3-methylpiperazine-1-carboxylate (200 mg, 1.00mmol) , 2-cyclopropylacetic acid (120 mg, 1.20 mmol) , EDCI (287mg, 1.50 mmol) and HOAT (340 mg, 2.50 mmol) in DCM (20 mL) was stirred at 0 , and DIPEA (0.70 mL, 4.00mmol) was added dropwise. After the addition, the mixture was stirred at rt for16 h and washed with water (10 mL × 2) . The organiclayer was dried over anhydrous Na2SO4 and concentrated.The residue was purified by silica gel chromatography eluted with Petroleumether/EtOAc (v/v) 2/1 to give (R) -tert-butyl 4-(2-cyclopropylacetyl) -3-methylpiperazine-1-carboxylate as colorless oil (260mg, 92) . 1H NMR (400 MHz, CDCl3): delta ppm 3.85-4.14 (m, 3H) , 3.31-3.55 (m, 1H) , 2.80-2.97 (m, 3H) , 2.30-2.33,2.20-2.23 (m, m, 0.5H, 1.5H) , 1.46 (s, 9H) , 1.15-1.24 (m, 3H) , 1.03-1.07 (m,1H) , 0.55-0.57 (m, 2H) , 0.15-0.18 (m, 2H) ., 163765-44-4

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

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

163765-44-4, (R)-1-Boc-3-Methylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a mixture of triphosgene (23 g, 75 mmol) in anhydrous DCM (250 mL) was added pyridine (18 g, 225 mmol) drop-wise followed by addition of tert-butyl (3R)-3-methylpiperazine-1-carboxylate (15 g, 75 mmol) at 0 C. The mixture was stirred overnight at RT. TLC showed the starting material had been consumed. The mixture was concentrated to afford Intermediate 8 as yellow solid, which was used without further purification., 163765-44-4

The synthetic route of 163765-44-4 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; LI, David Yunzhi; WANG, Jiabing; YANG, Zhenfan; ZENG, Qingbei; ZHANG, Xiaolin; US2014/255428; (2014); 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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

The compound (R) -3- methyl-piperazine-1-carboxylate (500mg, 2.5mmol) and triethylamine (700mg,6.3mmol) in methylene Dichloromethane (10 mL), and the conditions under 0 C, to this solution was addeddropwise methanesulfonyl chloride (0.39mL, 4.99mmol), stirred at rt for 8h, add Water (10mL × 3), dried overanhydrous Na 2 SO 4 organic phase was dried, the solvent was removed concentrate was subjected to columnchromatography (eluent: Petroleum ether / EtOAc (v / v) = 2/1), to give 444mg white solid: (R) -3- methyl-4-(methylsulfonyl) piperazine-1-carboxylate, yield: 63% ., 163765-44-4

163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

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.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

A mixture of (R) -tert-butyl 3-methylpiperazine-1-carboxylate (500 mg, 2.50 mmol) , propionic acid (0.22 mL, 3.00 mmol) , EDCI (718 mg, 3.74 mmol) and HOAT (850 mg, 6.24 mmol) in DCM (15 mL) was stirred at 0 , and DIPEA (1.7 mL, 9.99 mmol) was added dropwise. After the addition, the mixture was stirred at rt for 16 h and washed with water (10 mL × 2) . The organic layer was dried over anhydrous Na2SO4 and concentrated. The residue was purified by silica gel chromatography eluted with Petroleum ether/EtOAc (v/v) 2/1 to give (R) -tert-butyl 3-methyl-4-propionylpiperazine-1-carboxylate as colorless oil (630 mg, 95) .1H NMR (400 MHz, CDCl3) : delta ppm 4.76, 4.36 (m, m, 0.5H, 0.5H) , 4.00-3.94 (m, 1H) , 3.85-3.76 (m, 1H) , 3.53, 3.29 (m, m, 0.5H, 0.5H) , 2.98-2.96 (m, 1H) , 2.83-2.74 (m, 2H) , 2.34-2.26 (m, 2H) , 1.45 (s, 9H) , 1.13 (t, J 7.0 Hz, 6H) .

163765-44-4, 163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

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