水溶液中钯催化的Heck/氰基化串联反应合成3-氰甲基吲哚酮

Synthesis of 3-Cyanomethyl Oxoindoles via Palladium-Catalyzed Domino Heck/Cyanation Reaction in Water

3-氰甲基吲哚酮是一类重要的药物合成中间体,利用其氰基官能团的转化可以合成Horsfiline、Esermethole和Physostigmine等天然产物.发展了一种水溶液中的Heck/氰基化串联反应,可以绿色、简便地合成3-氰甲基吲哚酮类化合物,该方法与文献方法相比,不仅能够以绿色介质水代替有机溶剂,而且不需要添加碱作为缚酸剂,为3-氰甲基吲哚酮类化合物提供了一种绿色高效的合成新途径.

3-Cyanomethyl oxoindoles are a kind of important drug intermediates, which can be used to synthesize horsfiline, esermethole and physostigmine and other natural products via the conversion of cyano functional groups. A domino Heck/cyanation reaction in aqueous was developed to afford 3-cyanomethyl oxoindole compounds. This method, using green medium water instead of organic solvents, without any basic additives, provided a green and efficient new procedure for the synthesis of 3-cyanomethyl oxoindoles.