With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-08-2,1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.
A mixture of (S) -5- (1- ( (tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4- (difluoromethoxy) phenyl) oxazole-4-carboxylic acid (0.6 g, 1.28 mmol) , 1-tert-butyl 3-methyl piperazine-1, 3-dicarboxylate (376 mg, 1.54 mmol) , EDCI (368 mg, 1.92 mmol) and HOAT (435 mg, 3.20 mmol) in DCM (20 mL) was stirred at 0 , and DIPEA (0.89 mL, 5.12 mmol) was added dropwise. After the addition, the mixture was stirred at rt for 6 h and washed with saturated aqueous NaCl (15 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) 4/1 to give the title compound as a white solid (714 mg, 80) .1H NMR (400 MHz, CDCl3) : delta ppm 7.57 (s, 1H) , 7.52-7.54 (m, 1H) , 7.24-7.27 (m, 1H) , 6.72 (t, JF-H 75.0 Hz, 1H) , 5.21-5.28 (m, 1H) , 4.60-4.68 (m, 2H) , 3.99 (d, J 6.9 Hz, 2H) , 3.81 (s, 3H) , 3.24-3.29 (m, 1H) , 3.00-3.10 (m, 1H) , 1.52-1.57 (m, 3H) , 1.49 (s, 9H) , 1.44 (s, 9H) , 1.32-1.37 (m, 1H) , 0.68-0.73 (m, 2H) , 0.42-0.44 (m, 2H) and MS-ESI: m/z 695.3 [M+H] +.
129799-08-2, The synthetic route of 129799-08-2 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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