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AssigneesAscentage Pharma (Suzhou) Co., Ltd., Ascentage Pharma Group Corp Limited
InventorsJianfeng WEN, Jianyong CHEN, Yunlong ZHOU, Jianpeng FENG, Ming GUO, Tianzhu WU, Minmin CAI, Yu JING, Lingling JIAO
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Disclosed is a method for synthesizing N-(phenylsulfonyl)benzamide compound and intermediate thereof. The method comprises a method for synthesizing a compound 1, comprising conducting a Buchwald-Hartwig coupling reaction as shown below with compound A and compound B in a solvent and in the presence of a base and a palladium catalyst to obtain the compound 1; wherein R is C1-C8 alkyl. The present disclosure synthesizes three intermediate compounds required by the target compound and their preparation methods for the first time. Using the method disclosed in the present disclosure to synthesize the target compound 3 has the advantages of high yield, good purity, easy-to-obtain reaction raw materials, suitable for industrial production.
A method for synthesizing compound 1, comprising conducting a Buchwald-Hartwig coupling reaction as shown below with compound A and compound B in a solvent and in the presence of a base and a palladium catalyst to obtain compound 1;
A method for synthesizing compound 2, which refers to either method 1 or method 2:
A method for synthesizing compound 3, comprising conducting an amidation reaction as shown below with compound 2 and compound D in the presence of a condensing agent, a base and a catalyst to obtain compound 3;
A method for synthesizing the salt of compound A, comprising conducting a reaction as shown below with compound A-7 in a solvent and in the presence of an acid to obtain the salt of compound A;
A compound or a pharmaceutically acceptable salts thereof selected from one of the following:
Dependencies are inferred from the claim text.