Su Shikuan, Li Chunju, Jia Xueshun, Li Jian
Department of Chemistry, Innovative Drug Research Center, Shanghai University, 99 Shangda Road, Shanghai, 200444 (P. R. China), Fax: (+86) 21-66132408.
Chemistry. 2014 May 12;20(20):5905-9. doi: 10.1002/chem.201402576. Epub 2014 Apr 2.
A concise multicomponent reaction of isocyanide, α-substituted allenoate, and methyleneindolinone has been disclosed. This protocol provides a fast and straightforward approach to synthesize unusual tricyclic oxindoles in an efficient and atom-economic manner. Mechanistically, the present cycloaddition may proceed through a cascade sequence involving double Michael addition, double cyclization, double [1,5]-hydrogen shift, and group migration. The introduction of a special alkyl group to the allenoate is believed to play a key role in the cascade reaction. This method also features a broad substrate scope, which is particularly useful for the delivery of a large number of compounds.
已公开了异腈、α-取代的丙二烯酸酯和亚甲基吲哚酮的一种简洁多组分反应。该方法提供了一种快速且直接的途径,以高效且原子经济的方式合成不寻常的三环氧化吲哚。从机理上讲,当前的环加成反应可能通过一个涉及双迈克尔加成、双环化、双[1,5]-氢迁移和基团迁移的串联序列进行。据信在丙二烯酸酯上引入一个特殊的烷基在串联反应中起关键作用。该方法还具有广泛的底物范围,这对于大量化合物的合成特别有用。