文献类型：期刊文献

英文题名：PVP-I Catalyzed Oxidation of N-substituted Benzylamines to Benzamides

作者：Lu, Guangying[1];Yuan, Xinxin[1];Wang, Jian[1];Sun, Xue-Qin[1];Cao, Fu-Rong[1];Ren, Jiangmeng[1];Ke, Yanxiong[2];Mu, Xin[1];Zeng, Bu-Bing[1]

机构：[1]East China Univ Sci & Technol, Shanghia Frontiers Sci Ctr Optogenet Tech Cell Met, Sch Pharm, 130 Meilong Rd, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Engn Res Ctr Pharmaceut Proc Chem, Sch Pharm, 130 Meilong Rd, Shanghai 200237, Peoples R China

年份：2024

卷号：9

期号：1

外文期刊名：CHEMISTRYSELECT

收录：;WOS:【SCI-EXPANDED(收录号:WOS:001135006900001)】；

基金：This work was financially supported by Shanghai Frontiers Science Center of Optogenetic Techniques for Cell Metabolism (Shanghai Municipal Education Commission) and Natural Science Foundation of Shanghai (22ZR1416700).

语种：英文

外文关键词：PVP-I; Benzamides; Oxidation; TBHP; Enzalutamide

摘要：An oxidative transformation from N-substituted benzylamine into the corresponding benzamides was developed here using the oxidative system combined from the catalytic amount of PVP-I (polyinyl pyrrolidone) with TBHP. This newly developed method had the advantages of mild reaction conditions and broad substrate scope. The key intermediate of Enzalutamide as androgen receptor inhibitors was prepared using this catalytic condition starting from commercial available 2-fluoro-4-nitrobenzaldehyde with the yield of 78.5 % for three-step reactions.