Chemoselective One-Pot Synthesis of Functionalized Amino-azaheterocycles Enabled by COwareClick to copy article linkArticle link copied!
- Thomas A. Clohessy
- Alastair Roberts
- Eric S. Manas
- Vipulkumar K. Patel
- Niall A. Anderson
- Allan J. B. Watson
Abstract

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 Hedgehog and dual PI3K/mTOR inhibitors, which show enhanced physicochemical properties compared to their unsaturated counterparts.
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