Title:
PREPARATION METHODS FOR UPADACITINIB AND INTERMEDIATE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/242278
Kind Code:
A1
Abstract:
A method for synthesizing an intermediate of upadacitinib, comprising: (1) compound formula 1 undergoes an epoxidation reaction, an addition reaction, and a protection reaction to obtain compound formula 4; compound formula 4 reacts with an acetyl reagent to obtain compound formula 5; and then compound formula 5 reacts with a bromination reagent to obtain compound formula 6. A reaction formula is as follows: formula (1), wherein G is the protecting group of a nitrogen atom or a trifluoroethylformamide group, and R is the protecting group of a hydroxyl group.
Inventors:
RUAN JING (CN)
YAN GONGCHAO (CN)
RUAN XIAONA (CN)
ZHANG WEI (CN)
ZHANG XINXIN (CN)
YAN GONGCHAO (CN)
RUAN XIAONA (CN)
ZHANG WEI (CN)
ZHANG XINXIN (CN)
Application Number:
PCT/CN2022/080533
Publication Date:
November 24, 2022
Filing Date:
March 13, 2022
Export Citation:
Assignee:
SHANGHAI DINGYA PHARMACEUTICAL CHEMICALS CO LTD (CN)
International Classes:
C07D207/09; C07D487/14
Domestic Patent References:
| WO2020043033A2 | 2020-03-05 |
Foreign References:
| CN111217819A | 2020-06-02 | |||
| CN110615753A | 2019-12-27 | |||
| CN105451773A | 2016-03-30 | |||
| CN101087778A | 2007-12-12 |
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