Title:
METHOD FOR PREPARING EZETIMIBE AND INTERMEDIATE COMPOUND THEREOF
Document Type and Number:
WIPO Patent Application WO/2017/140251
Kind Code:
A1
Abstract:
Provided are a method for preparing ezetimibe and an intermediate compound thereof. Provided is an economic method which is new, is easy to realize in industry, only includes very few steps and is established on a new intermediate. In the method, a compound of 1-(4-3(R)-[3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) is produced by the steps of performing a Mannich addition reaction of an acidylated oxazolidinone compound as shown by formula II with a protected imine compound as shown by formula III, then cyclizing, hydrolyzing, removing protecting groups, and reducing. The preparation method is concise in steps, high in reaction stereoselectivity, high in yield, low in cost, simple and convenient in operation, and can easily realize industrial production.
Inventors:
ZHANG XINI (US)
ZHOU TAO (CN)
XIONG ZHIGANG (CN)
ZHOU TAO (CN)
XIONG ZHIGANG (CN)
Application Number:
PCT/CN2017/073787
Publication Date:
August 24, 2017
Filing Date:
February 16, 2017
Export Citation:
Assignee:
CHANGZHOU FANGNAN PHARMACEUTICALS LTD (CN)
International Classes:
C07D205/08; C07D405/06; C07D413/06
Domestic Patent References:
| WO1997045406A1 | 1997-12-04 |
Foreign References:
| CN101346349A | 2009-01-14 | |||
| CN1329592A | 2002-01-02 | |||
| CN1131416A | 1996-09-18 |
Attorney, Agent or Firm:
SHANGHAI KAIJI INTELLECTUAL PROPERTY AGENT CO., LTD. (CN)
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