叔烯酰胺对吲哚和胺的直接烷基化反应：易于获得具有药物活性的 2-氧代-1-吡咯烷类似物。
Direct alkylation of indoles and amines by tert-enamides: facile access to pharmaceutically active 2-oxo-1-pyrrolidine analogues.
机构信息
Key Laboratory of Organic Synthesis of Jiangsu Province, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou, China.
出版信息
Org Biomol Chem. 2011 Aug 21;9(16):5659-69. doi: 10.1039/c1ob05546a. Epub 2011 Jun 24.
Direct alkylation of indoles and amines by tertiary enamides for the synthesis of pharmaceutically active 2-oxo-1-pyrrolidine analogues was described. With only a 0.5 mol% catalyst loading, molecular iodine was demonstrated to be efficiently enough to promote the reaction under neat condition. Only Markovnikov addition product was obtained indicating that the reactions proceeded with excellent regioselectivity.
本文描述了通过叔烯酰胺对吲哚和胺的直接烷基化反应来合成具有药用活性的 2-氧代-1-吡咯烷类似物。在 0.5mol%的催化剂负载量下，仅需分子碘就能有效地促进在无溶剂条件下的反应。仅得到 Markovnikov 加成产物，表明反应具有极好的区域选择性。
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