钯催化 N-酰基-o-炔基苯胺高区域和立体选择性合成 4-亚烷基-4H-3,1-苯并恶嗪。
Palladium-catalyzed highly regio- and stereoselective synthesis of 4-alkylidene-4H-3,1-benzoxazines from N-acyl-o-alkynylanilines.
机构信息
Department of Chemistry, Faculty of Science, Tokyo University of Science, Tokyo, Japan.
出版信息
Org Lett. 2011 Mar 4;13(5):1098-101. doi: 10.1021/ol103130s. Epub 2011 Feb 3.
PMID:21291205
Abstract
The highly regio- and stereoselective 6-exo-dig mode cyclization of N-acyl-o-alkynylanilines producing 4-alkylidene-3,1-benzoxazines occurred unpredictably by use of a proper catalyst [Pd(OAc)(2)] and an effective additive (acetic acid) under suitable reaction conditions.
摘要
在适当的反应条件下，使用合适的催化剂[Pd(OAc)(2)]和有效的添加剂（醋酸），N-酰基-o-炔基苯胺发生高度区域和立体选择性的 6-endo-dig 模式环化反应，生成 4-亚烷基-3,1-苯并恶嗪。
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