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1. (WO2018028679) POST-PROCESSING METHOD FOR MIRABEGRON INTERMEDIATE

Pub. No.:    WO/2018/028679    International Application No.:    PCT/CN2017/097117
Publication Date: Fri Feb 16 00:59:59 CET 2018 International Filing Date: Sat Aug 12 01:59:59 CEST 2017
IPC: C07C 213/02
C07C 213/10
C07C 215/30
Applicants: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD.
浙江华海药业股份有限公司
Inventors: DU, Xiaoqiu
杜小秋
LIU, Jiegen
刘节根
LIN, Yanxin
林炎鑫
Title: POST-PROCESSING METHOD FOR MIRABEGRON INTERMEDIATE
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: