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Title:
POST-PROCESSING METHOD FOR MIRABEGRON INTERMEDIATE
Document Type and Number:
WIPO Patent Application WO/2018/028679
Kind Code:
A1
Abstract:
A post-processing method for a Mirabegron intermediate, comprising the following steps: with a Mirabegron carbonyl of formula I serving as a reaction raw material, the carbonyl therein is reduced via a reduction reaction under the effects of a borane reagent; when the reaction is completed, a mixture is produced by cooling and a quenching reaction; the mixture is vacuum distilled, cooled, and added with water and an organic solvent; a strong base is used to regulate the pH value, stirred until both the water layer and the organic layer are clear, then kept still for stratification; and an organic phase is separated for later use. The method requires inexpensive raw material and reagent, provides great economic effects, employs the strong base instead of a carbonate, reduces the amount of base and water used in post-processing, reduces gaseous, liquid, and solid wastes, prevents an insoluble inorganic salt from being produced, and is suitable for industrialized production. The structures of formula I and formula II are as follows:

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Inventors:
DU XIAOQIU (CN)
LIU JIEGEN (CN)
LIN YANXIN (CN)
Application Number:
PCT/CN2017/097117
Publication Date:
February 15, 2018
Filing Date:
August 11, 2017
Export Citation:
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Assignee:
ZHEJIANG HUAHAI PHARM CO LTD (CN)
International Classes:
C07C213/02; C07C213/10; C07C215/30
Domestic Patent References:
WO2015162536A12015-10-29
WO2016024284A22016-02-18
WO2014132270A22014-09-04
WO2004041276A12004-05-21
WO2015096604A12015-07-02
Foreign References:
CN106278909A2017-01-04
CN104016943A2014-09-03
CN104230840A2014-12-24
CN105481705A2016-04-13
CN104016877A2014-09-03
Attorney, Agent or Firm:
PATENTSINO IP FIRM (CN)
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