3a-溴六氢吡咯并[2,3-b]吲哚支架 C3a 叔碳原子上的亲核取代反应容易发生。
Facile nucleophilic substitution at the C3a tertiary carbon of the 3a-bromohexahydropyrrolo[2,3-b]indole scaffold.
机构信息
Cancer Research UK Protein-Protein Interactions Drug Discovery Research Group, School of Pharmacy, University of London, 29-39 Brunswick Square, London, UK.
出版信息
Org Biomol Chem. 2010 Dec 7;8(23):5294-303. doi: 10.1039/c0ob00327a. Epub 2010 Sep 20.
PMID:20856944
Abstract
The synthesis of 3a-substituted hexahydropyrrolo[2,3-b]indole derivatives via nucleophilic substitution at the C3a position is reported. Nitrogen-, oxygen-, sulfur-, fluoro- and carbon-based nucleophiles have been employed, using both conventional organic solvents and ionic liquids. The C3a-substituted derivatives were obtained in good to excellent yields.
摘要
本文报道了通过 C3a 位的亲核取代反应合成 3a-取代的六氢吡咯并[2,3-b]吲哚衍生物。使用了包括传统有机溶剂和离子液体在内的多种氮、氧、硫、氟和碳亲核试剂，得到了 C3a 取代衍生物，产率良好到优秀。
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