Tandem Reduction, Ammonolysis, Condensation, and Deamination Reaction for Synthesis of Benzothiadiazines and 1--1 H-benzimidazoles

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作者: Xiao Yu, Zhihong Ma, Wenjing Zhu, Hongyan Liu, Zenghui Zhang, Yi Liu, Mei Zhang, Jinbo Zhao, Pengfei Zhang, Chengcai Xia

作者单位: Affiliations ¹ Institute of Pharmacology, Pharmacy College, Shandong First Medical University & Shandong Academy of Medical Sciences, Tai'an 271016, China. ² Biotalk Co., Ltd., Shanghai 200092, China. ³ College of Material, Chemistry and Chemical Engineering, Key Laboratory of Organosilicon Chemistry and Material Technology, Ministry of Education, Hangzhou Normal University, Hangzhou 311121, China.

摘要: A novel route for a SnCl-promoted tandem reduction, ammonolysis, condensation, and deamination reaction which uses nitrile and 2-nitro-N-phenylbenzenesulfonamide/N-benzenesulfonamide to synthesize derivatives of benzothiadiazine/1--1H-benzimidazole has been developed. The method features convenient operation and good functional group tolerance. In addition, it employs unsensitive and inexpensive SnCl/i-PrOH as the reaction reagent and provides a direct approach for the synthesis of pharmaceutica...更多; A novel route for a SnCl-promoted tandem reduction, ammonolysis, condensation, and deamination reaction which uses nitrile and 2-nitro-N-phenylbenzenesulfonamide/N-benzenesulfonamide to synthesize derivatives of benzothiadiazine/1--1H-benzimidazole has been developed. The method features convenient operation and good functional group tolerance. In addition, it employs unsensitive and inexpensive SnCl/i-PrOH as the reaction reagent and provides a direct approach for the synthesis of pharmaceutically important targets.收起

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