Title:
METHOD FOR PREPARING TAZOBACTAM KEY INTERMEDIATE, 6α-BROMOPENICILLANIC SULFOXIDE ACID DIPHENYLMETHYL ESTER
Document Type and Number:
WIPO Patent Application WO/2019/100544
Kind Code:
A1
Abstract:
A novel method for preparing a key intermediate, a 6α-bromopenicillanic sulfoxide acid diphenylmethyl ester, in tazobactam analysis. The method comprises the following steps: dissolving a 6α-bromopenicillanic sulfoxide acid in an organic solvent, adding diphenyldiazomethane, evaporating the solvent under reduced pressure after complete reaction, performing extraction with the organic solvent, washing an organic layer with saturated brine, and after drying with anhydrous sodium sulfate, evaporating the solvent under reduced pressure to obtain a crude product. The crude product is recrystallized or washed by beating with the organic solvent, and thus a 6α-bromopenicillanic sulfoxide acid diphenylmethyl ester can be obtained. Compared with a conventional method for producing esters with a condensing agent, such as DCC, the method avoids the problem of a difficulty in removal of reaction by-products. Compared with using a benzophenone hydrazone/KI/peracetic acid system for esterification, the method simplifies operations, reduces by-products, improves the purity of final products, and is more conducive to industrial production.
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Inventors:
GAO FENG (CN)
Application Number:
PCT/CN2018/000379
Publication Date:
May 31, 2019
Filing Date:
November 05, 2018
Export Citation:
Assignee:
BEIJING RUNWELL BIOTEPHARM CO LTD (CN)
BEIJING MEDIKING BIOPHARM CO LTD (CN)
BEIJING MEDIKING BIOPHARM CO LTD (CN)
International Classes:
C07D499/865; C07D499/08
Foreign References:
| CN106632397A | 2017-05-10 | |||
| CN108264519A | 2018-07-10 |
Attorney, Agent or Firm:
TIANJIN JIEYING PATENT AND AGENT LTD. (CN)
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