Title:
METHOD FOR PREPARING GLECAPREVIR SYNTHETIC INTERMEDIATE AND AMINE SALT THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/084740
Kind Code:
A1
Abstract:
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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Inventors:
YE FANGGUO (CN)
LONG SHUANGXI (CN)
LIU QINGQING (CN)
LONG SHUANGXI (CN)
LIU QINGQING (CN)
Application Number:
PCT/CN2017/108453
Publication Date:
May 09, 2019
Filing Date:
October 31, 2017
Export Citation:
Assignee:
SHANGHAI TWISUN BIO PHARM CO LTD (CN)
International Classes:
C07C271/34; C07C41/03; C07C43/196; C07C69/14; C07C209/00; C07C211/07; C07C269/00
Foreign References:
| CN103209703A | 2013-07-17 | |||
| CN105849118A | 2016-08-10 | |||
| US9809576B1 | 2017-11-07 |
Attorney, Agent or Firm:
BEIJING GAOWO LAW FIRM (CN)
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