The synthesis of novel heteroaryl-fused 7,8,9,10-tetrahydro-6H-azepino[1,2-a]indoles, 4-oxo-2,3-dihydro-1H-[1,4]diazepino[1,7-a]indoles and 1,2,4,5-tetrahydro-[1,4]oxazepino[4,5-a]indoles. Effective inhibitors of HCV NS5B polymerase
作者:Min Ding、Feng He、Michael A. Poss、Karen L. Rigat、Ying-Kai Wang、Susan B. Roberts、Dike Qiu、Robert A. Fridell、Min Gao、Robert G. Gentles
DOI:10.1039/c1ob05525a
日期:——
Three synthetic approaches have been developed that allow efficient access to novel heteroaryl fused indole ring systems, including: 7,8,9,10-tetrahydro-6H-azepino[1,2-a]indoles, 4-oxo-2,3-dihydro-1H-[1,4]diazepino[1,7-a]indoles and 1,2,4,5-tetrahydro-[1,4]oxazepino[4,5-a]indoles. Each strategy is fully exemplified and the relative merits and limitations of the approaches are discussed. The hepatitis C virus (HCV) non-structural 5B (NS5B) polymerase inhibitory activities of select examples from each molecular class are briefly presented.
已经开发了三种合成方法,可以有效地获得新型杂芳基稠合吲哚环系统,包括:7,8,9,10-四氢-6H-氮杂[1,2-a]吲哚、4-氧代-2,3-二氢-1H-[1,4]二氮杂[1,7-a]吲哚和1,2,4,5-四氢-[1,4]氧氮杂[4,5-a]吲哚。每个策略都得到了充分的例证,并讨论了这些方法的相对优点和局限性。简要介绍了每个分子类别中选定实例的丙型肝炎病毒 (HCV) 非结构 5B (NS5B) 聚合酶抑制活性。