Chemoselective One-Pot Synthesis of Functionalized Amino-azaheterocycles Enabled by COware
作者:Thomas A. Clohessy、Alastair Roberts、Eric S. Manas、Vipulkumar K. Patel、Niall A. Anderson、Allan J. B. Watson
DOI:10.1021/acs.orglett.7b03214
日期:2017.12.1
Functionalized bicyclic amino-azaheterocycles are rapidly accessed in a one-pot cross-coupling/reduction sequence enabled by the use of COware. Incompatible reagents are physically separated in a single reaction vessel to effect two chemoselective transformations—Suzuki–Miyaura cross-coupling and heteroarene reduction. The developed method allows access to novel heterocyclic templates, including semisaturated
功能化的双环氨基氮杂环化合物可以通过使用COware实现的一锅式交叉偶联/还原序列快速访问。不相容的试剂在一个反应容器中进行物理分离,以实现两个化学选择性转化-Suzuki-Miyaura交叉偶联和杂芳烃还原。所开发的方法允许访问新型杂环模板,包括半饱和刺猬和双PI3K / mTOR抑制剂,与不饱和对应物相比,它们显示出增强的理化性质。