Process Development Overcomes a Challenging Pd-Catalyzed C–N Coupling for the Synthesis of RORc Inhibitor GDC-0022

Lauren E. Sirois,David Lao,Jie Xu,Remy Angelaud,Jerry Tso,Brandon Scott,Paroma Chakravarty,Sushant Malhotra,Francis Gosselin

Process Development Overcomes a Challenging Pd-Catalyzed C–N Coupling for the Synthesis of RORc Inhibitor GDC-0022

2020

Lauren E. Sirois
David Lao
Jie Xu
Remy Angelaud
Jerry Tso
Brandon Scott
Paroma Chakravarty
Sushant Malhotra
Francis Gosselin

Process development for a multi-kilogram-scale synthesis of GDC-0022, an inhibitor of retinoic acid receptor-related orphan receptor γ (RORc), is described. Delivery of the active pharmaceutical in...

Keywords:

Orphan receptor
Catalysis
RAR-related orphan receptor gamma
Reaction progress kinetic analysis
Organic chemistry
Combinatorial chemistry
Retinoic acid
process development
Chemistry

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