专利名称 | METHOD FOR PREPARING GLECAPREVIR SYNTHETIC INTERMEDIATE AND AMINE SALT THEREOF | ||
申请号 | WOCN17108453 | 申请日 | |
公开(公告)号 | WO2019084740A1 | 公开(公告)日 | |
申请(专利权)人 | SHANGHAI TWISUN BIO PHARM CO LTD | 发明人 | YE Fangguo; LONG Shuangxi; LIU Qingqing |
专利来源 | 国家知识产权局 | 转化方式 | |
摘要 |
Disclosed is a method for preparing a Glecaprevir synthetic intermediate. An epoxy cyclopentane is used as a starting material to carry out a ring opening reaction to form 2-hydroxy-1-propenyloxycyclopentane, the same being acetylated to obtain 2-acetoxy-1-propenyloxycyclopentane. The 2-acetoxy-1-propenyloxycyclopentane is subjected to resolution and then activation and amino condensation in sequence to obtain a Glecaprevir synthetic intermediate. The disclosed method has fewer reaction steps, and higher yield. The total yield is higher than 30% on average and is much higher than the 10% yields in the prior art. The method is also low in cost, environmentally friendly, has mild in reaction conditions, is simple to operate, and suitable for industrialization. Further disclosed is a preparation method for a Glecaprevir synthetic intermediate amine salt likewise featuring high yields, mild reaction conditions, and simple operation. |
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