Shirakawa Seiji, Kobayashi Shu
Graduate School of Pharmaceutical Sciences, The University of Tokyo, The HFRE Division, ERATO, Japan Science and Technology Agency (JST), Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Org Lett. 2006 Oct 12;8(21):4939-42. doi: 10.1021/ol062031q.
[reaction: see text] The carboxylic acid catalyzed three-component aza-Friedel-Crafts reactions of aldehydes, primary amines, and indoles in water have been developed. The aza-Friedel-Crafts products could be easily transformed to various 3-substituted indoles including biologically active compounds. This system offers a novel efficient method for the synthesis of 3-substituted indoles.
[反应:见正文] 已开发出羧酸催化的醛、伯胺和吲哚在水中的三组分氮杂傅-克反应。氮杂傅-克产物可轻松转化为各种3-取代吲哚,包括生物活性化合物。该体系为3-取代吲哚的合成提供了一种新颖有效的方法。