Process Development for a Key Synthetic Intermediate of LY2140023, a Clinical Candidate for the Treatment of Schizophrenia

Waser, Mario; D. Moher, Eric; S. K. Borders, Sandy; M. Hansen, Marvin; W. Hoard, David; E. Laurila, Michael; E. LeTourneau, Michael; D. Miller, Richard; Laurie Phillips, M.; A. Sullivan, Kevin; A. Ward, Jeffrey; Xie, Chaoyu; A. Bye, Cheryl; Leitner, Tanja; Herzog-Krimbacher, Brigitte; Kordian, Marcus; Müllner, Martin

doi:10.1021/op100325h

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Process Development for a Key Synthetic Intermediate of LY2140023, a Clinical Candidate for the Treatment of Schizophrenia

Published in Organic Process Research & Development • Sep 27, 2011

Authors:

Mario Waser

Eric D. Moher

Sandy S. K. Borders

Abstract

To fuel clinical development of the experimental CNS medicine LY2140023, we developed a scalable route for the multistep synthesis of a pivotal synthetic intermediate. The core of the conformationally restricted glutamic acid-based amino acid analogue was built via a Rh-catalyzed cyclopropanation of...

Subject

Regioselectivity

Combinatorial chemistry

Hydroboration

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