Chemoselective One-Pot Synthesis of Functionalized Amino-azaheterocycles Enabled by COware
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.
Clohessy, Thomas A.,Roberts, Alastair,Manas, Eric S.,Patel, Vipulkumar K.,Anderson, Niall A.,Watson, Allan J. B.
p. 6368 - 6371
(2017/12/08)
INHIBITORS OF THE HEDGEHOG PATHWAY
The present invention is directed to a compound of Formula (I) or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula (I) to treat cancer.
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(2008/12/07)
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