Document Type

Article

Department or Administrative Unit

Chemistry

Publication Date

2-28-2020

Abstract

C1 benzylated isoquinoline derivatives constitute the core of benzylisoquinoline alkaloids (BIAs). However, their C4 congeners remain elusive. Here, we describe a diastereoselective, catalytic, and modular C(sp3)–C(sp3) coupling protocol wherein β-amino sp3 C–H bonds of readily affordable vicinally functionalized dihydroisoquinolones are replaced by sp3 C–benzyl bonds. The method provides expedient access to C4 quaternary and homobenzylic dihydroisoquinolones, which are attractive fragments for potential drug discovery.

Comments

This article was originally published in RSC Advances. The full-text article from the publisher can be found here.

Journal

RSC Advances

Creative Commons License

Creative Commons Attribution-Noncommercial 4.0 License
This work is licensed under a Creative Commons Attribution-Noncommercial 4.0 License

Rights

© The Royal Society of Chemistry 2020

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