Title:
METHOD FOR SYNTHESIZING KEY CHIRAL INTERMEDIATE OF UPADACITINIB
Document Type and Number:
WIPO Patent Application WO/2023/029236
Kind Code:
A1
Abstract:
The present application provides a method for synthesizing a key intermediate II-a of upadacitinib. The asymmetric hydrogenation of unsaturated carboxylic acid I-a can be catalyzed by means of Ru(OAc)2-(R)-OSPD to synthesize chiral carboxylic acid II-a, the chiral carboxylic acid II-a can form a salt together with tert-butylamine, and IV-a having high optical purity can be obtained after recrystallization. According to the method provided in the present application, an asymmetric hydrogenation catalyst has high catalytic efficiency and high enantioselectivity, and the operation is simple and convenient, thus facilitating industrial production.
Inventors:
ZHENG LONGSHENG (CN)
LIU CHUANGJI (CN)
DING XIAOBING (CN)
ZHAO JINHUI (CN)
LIU CHUANGJI (CN)
DING XIAOBING (CN)
ZHAO JINHUI (CN)
Application Number:
PCT/CN2021/132941
Publication Date:
March 09, 2023
Filing Date:
November 25, 2021
Export Citation:
Assignee:
SHENZHEN CATALYS TECH CO LTD (CN)
International Classes:
C07D207/16; C07B53/00; C07C209/00; C07C211/07
Domestic Patent References:
| WO2019153203A1 | 2019-08-15 |
Foreign References:
| CN111217819A | 2020-06-02 | |||
| CN109503659A | 2019-03-22 | |||
| CN110128471A | 2019-08-16 |
Attorney, Agent or Firm:
SHENZHEN LANFENG SHENGSHI INTELLECTUAL PROPERTY AGENCY CO., LTD (CN)
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