A kind of preparation method of cefcapene hydrochloride intermediate bcn

A technology of cefcapene hydrochloride and intermediates, applied in organic chemistry and other fields, can solve the problems of long industrial routes and low purity
CN109678887BActive Publication Date: 2020-08-14湖北凌晟药业股份有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
湖北凌晟药业股份有限公司
Publication Date
2020-08-14

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Abstract

The invention provides a preparation method of cefcapene pivoxil hydrochloride intermediate BCN, and belongs to the technical field of organic synthesis. Mixed anhydride BAPA prepared by a mixed anhydride preparation reaction and D-7-ACA-MG salt can be subjected to a condensation reaction, and the cefcapene pivoxil hydrochloride intermediate BCN is obtained by carbamoylation reaction and salt formation crystallization. The preparation method has short process route, high product purity and low cost, and is suitable for industrial production. Data of the embodiment shows that the prepared cefcapene pivoxil hydrochloride intermediate BCN can have purity as high as 98.84% and yield as high as 91.99%.
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Description

technical field

[0001] The invention belongs to the technical field of organic synthesis, in particular to a preparation method of cefcapene hydrochloride intermediate BCN. Background technique

[0002] Cefcapene pivoxil hydrochloride is the fourth generation of oral cephalosporin antibiotics. Cefcapene pivoxil hydrochloride intermediate (BCN) is a key intermediate for the synthesis of cefcapene pivoxil hydrochloride and is also a precursor raw material, hereinafter referred to as BCN. The core D-7-ACA and the side chain BAPA are prepared by the mixed anhydride preparation reaction and the subsequent treatment process. After BCN is modified, various cefcapene hydrochloride analogues can also be obtained. The existing BCN synthesis methods generally have low purity. The lack of long industrial routes. As the prior art discloses the synthesis of thiazole acetic acid (BAPA) through reactions such as condensation, cyclization, and introduction of protecting groups of 4-chloroac...

Claims

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