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Multikilogram Synthesis of a Potent Dual Bcl-2/Bcl-xL Antagonist. 2. Manufacture of the 1,3-Diamine Moiety and Improvement of the Final Coupling Reaction

Authors :
Stéphane Le Roux
Sandrine Baillard
Olivier Russo
Christophe Hardouin
François Barière
Anthony Craquelin
Mathieu Grandjean
Christine Penloup
Solenn Janvier
Source :
Organic Process Research & Development. 24:670-685
Publication Year :
2019
Publisher :
American Chemical Society (ACS), 2019.

Abstract

This paper describes the synthesis of kilogram quantities of the sulfonamide moiety 3 involved in a coupling reaction with acid moiety 2 to provide batches of drug candidate 1 for preclinical studi...

Details

ISSN :
1520586X and 10836160
Volume :
24
Database :
OpenAIRE
Journal :
Organic Process Research & Development
Accession number :
edsair.doi...........9dd10adf791c4b850e0120fa8859053e
Full Text :
https://doi.org/10.1021/acs.oprd.9b00367