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 (250 mg, 1.25 mmol) , cyclopropanecarboxylic acid (130 mg, 1.50 mmol) , EDCI (480 mg, 2.50 mmol) and HOAT (254 mg, 1.87 mmol) in DCM (10 mL) was stirred at 0 , and DIPEA (0.65 mL, 3.74 mmol) was added dropwise. After the addition, the mixture was stirred at rt for 10 h and washed with water (10 mL × 3) . 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 4- (cyclopropanecarbonyl) -3-methylpiperazine-1-carboxylate as colorless oil (310 mg, 93) .1H NMR (400 MHz, CDCl3) : delta ppm 4.24-4.50 (m, 1H) , 3.78-4.07 (m, 2H) , 2.90-3.41 (m, 3H) , 2.81 (s, 6H) , 1.50 (s, 9H) , 1.12-1.36 (m, 4H) , 0.96-1.05 (m, 2H) , 0.74-0.82 (m, 2H) and MS-ESI: m/z 213.10 [M-55] +.
163765-44-4, The synthetic route of 163765-44-4 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;,
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