Title:
PREPARATION OF 4-BROMO-2-(4'-ETHOXY-BENZYL)-1-CHLOROBENZENE
Document Type and Number:
WIPO Patent Application WO/2022/116507
Kind Code:
A1
Abstract:
The present invention is aimed at providing a method for synthesizing 4-bromo-2-(4'-ethoxy-benzyl)-1-chlorobenzene. The method is in shorter in step and more environmentally friendly, and provides a more effective synthesis strategy for the production of a key intermediate of SGLT-2 inhibitor drugs, such as Dapagliflozin, Sotagliflozin, and Ertugliflozin. The method comprises: selecting 2-chlorine-5-bromobenzoic acid and phenetole, completing a direct acylation reaction under the presence of trifluoroacetic anhydride by using boron trifluoride etherate as a catalyst, adding triethylsilane without treatment, and performing one-pot reaction to obtain a target compound, i.e., 4-bromo-2-(4'-ethoxy-benzyl)-1-chlorobenzene.
Inventors:
HU LIN (CN)
XU TAO (CN)
QIU XIAOLONG (CN)
LI XIAOYUE (CN)
ZUO ZHIWEI (CN)
LIU WENBO (CN)
CHU LINGLING (CN)
YUAN XIMENG (CN)
ZOU PING (CN)
XU TAO (CN)
QIU XIAOLONG (CN)
LI XIAOYUE (CN)
ZUO ZHIWEI (CN)
LIU WENBO (CN)
CHU LINGLING (CN)
YUAN XIMENG (CN)
ZOU PING (CN)
Application Number:
PCT/CN2021/099079
Publication Date:
June 09, 2022
Filing Date:
June 09, 2021
Export Citation:
Assignee:
WISDOM PHARMACEUTICAL CO LTD (CN)
International Classes:
C07C41/30; B01J31/04; B01J31/22; C07C43/225
Foreign References:
| CN112500267A | 2021-03-16 | |||
| CN110396040A | 2019-11-01 | |||
| CN105061373A | 2015-11-18 | |||
| CN111662166A | 2020-09-15 |
Attorney, Agent or Firm:
CHANGZHOU BAIYETENGFEI PATENT AGENCY (GENERAL PARTNERSHIP) (CN)
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