With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.474711-89-2,Piperazine-1-carboxamide hydrochloride,as a common compound, the synthetic route is as follows.,474711-89-2
A mixture of (S) -2- (3- (benzyloxy) -4- (difluoromethoxy) phenyl) -5- (1- ( (tert-butoxy carbonyl) amino) ethyl) oxazole-4-carboxylic acid (300 mg, 0.595 mmol) , EDCI (171 mg, 0.892 mmol) and HOAT (121 mg, 0.892 mmol) in DCM (20 mL) was stirred at rt for 30 min, and piperazine-1-carboxamide hydrochloride (200 mg, 0.892 mmol) was added, and then DIPEA (1.5 mL, 9.52 mmol) was added dropwise at 0 . After the addition, the mixture was stirred at rt for 10 h and washed with water (25 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) 1/1 to give the title compound as a white solid (176 mg, 48) .1H NMR (400 MHz, CDCl3) : delta ppm 7.66 (d, J 2.0 Hz, 1H) , 7.61 (d, J1 8.4 Hz, J2 2.0 Hz, 1H) , 7.36-7.50 (m, 5H) , 7.29 (d, J 8.4 Hz, 1H) , 6.66 (t, JF-H 74.4 Hz, 1H) , 5.25-5.28 (m, 1H) , 5.25 (s, 2H) , 4.56 (s, 2H) , 3.83-4.00 (m, 4H) , 3.53-3.55 (m, 4H) , 1.57 (d, J 6.8 Hz, 3H) , 1.44 (s, 9H) and MS-ESI: m/z 616.30 [M+H] +.
The synthetic route of 474711-89-2 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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