Affiliation:
1. School of Pharmacy, Fudan University
2. Shanghai Center for Drug Discovery & Development
Abstract
Silver-catalyzed on-water intramolecular cyclization of acetylenic free amines is reported, which affords 7-azaindoles in good to excellent yields. Neither strong base/acid catalysts nor N-substituted substrates are required to achieve this cycloisomerization. Hydrogen bonds between water medium and the substrates play an important role in improving chemical reactivity and regioselectivity. Furthermore, the on-water reaction is extendable to acetylenic amides for isoquinolone synthesis.
Funder
National Basic Research Program of China, 973 Program
Science and Technology Commission of Shanghai Municipality
Subject
Organic Chemistry,Catalysis
Cited by
17 articles.
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