METHOD FOR PREPARING 5-BROMO-2-CHLORO-BENZOIC ACID AS RAW MATERIAL IN HYPOGLYCEMIC DRUG SYNTHESIS

Title:

METHOD FOR PREPARING 5-BROMO-2-CHLORO-BENZOIC ACID AS RAW MATERIAL IN HYPOGLYCEMIC DRUG SYNTHESIS

Document Type and Number:

WIPO Patent Application WO/2023/019849

Kind Code:

A1

Abstract:

The present invention relates to a method for preparing 5-bromo-2-chloro-benzoic acid as a raw material in hypoglycemic drug synthesis and the use thereof. Specifically, in the present invention, a 5-bromo-2-aminobenzoic acid derivative is used as a starting raw material, and 5-bromo-2-chloro-benzoic acid is prepared by two steps of diazotization and chlorination and hydrolysis reaction. A resulting product has few isomer impurities, the reaction yield is high, the purity is good, the cost is low, and the present invention is suitable for industrial production. The present invention also relates to the use of 5-bromo-2-amino-benzoic acid in the preparation of anti-diabetic drugs.

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Inventors:

LI YUNFENG (CN)
ZHENG ZHIGUO (CN)

Application Number:

PCT/CN2021/141256

Publication Date:

February 23, 2023

Filing Date:

December 24, 2021

Export Citation:

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Assignee:

ZHEJIANG AUSUN PHARMACEUTICAL CO LTD (CN)

International Classes:

C07C51/09; C07C63/70; C07C227/18; C07C229/56; C07C41/18; C07C43/225

Domestic Patent References:

WO2003099836A1	2003-12-04
WO2005092877A1	2005-10-06

Foreign References:

CN113773194A	2021-12-10
CN113801010A	2021-12-17
CN113912487A	2022-01-11
CN104086361A	2014-10-08
CN105622382A	2016-06-01
CN107954852A	2018-04-24
CN110105193A	2019-08-09
CN110590541A	2019-12-20
CN110002989A	2019-07-12
CN108250060A	2018-07-06
CN111925289A	2020-11-13
CN112979448A	2021-06-18

Other References:

YE FEI, GAO REN-XIAO, SHEN NING, DING ZHI-XIN, REN ZENG-GANG, LIU QIAN-FENG: "Synthesis of 2-chloro-5-iodobenzoic acid", YINGYONG-HUAGONG = APPLIED CHEMICAL INDUSTRY, YINGYONG HUAGONG ZAZHISHE, CN, vol. 40, no. 8, 28 August 2011 (2011-08-28), CN , pages 1479 - 1480, XP093036353, ISSN: 1671-3206, DOI: 10.16581/j.cnki.issn1671-3206.2011.08.035

Attorney, Agent or Firm:

ZHONGZI LAW OFFICE (CN)

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