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苯乙烯类吲唑衍生物是一类重要的类胰岛素生长因素1受体抑制剂。本文介绍了它的两种合成原料:6-氯-3-甲基吲唑和6-氟-3-羰甲基吲唑的合成方法,并对以邻卤苯羰基类化合物为原料生成苯腙再分子内环化和吲哚的重氮化反应这两种方法进行了改进。改进后的方法产率大大提高,反应时间缩短,后处理简化,更利于吲唑类化合物的大规模生产,对吲唑的工业化生产和医药行业具有重要的意义。
Styrenic indazole derivatives are a class of important insulin like growth factor 1 receptor inhibitors. This article describes the synthesis of two of its raw materials: 6-chloro-3-methylindazole and 6-fluoro-3-carbonylmethylindazole, and to orthohalophenyl carbonyl compounds as raw materials to produce phenylhydrazone Both intramolecular cyclization and indole diazotization have been improved. The improved method greatly improves the yield, the reaction time is shortened, and the post-treatment is simplified, which is more conducive to the large-scale production of indazole compounds and has important meanings for the industrialized production of indazole and the pharmaceutical industry.