Sep 2021 News Brief introduction of Piperazine-1-carboxamide hydrochloride

The synthetic route of 474711-89-2 has been constantly updated, and we look forward to future research findings.

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;,
Piperazine – Wikipedia
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