Process Development of a Tricyclic Diazepine-Based IDH1 Mutant Inhibitor
Matthew L. Maddess,
Ed Cleator,
Mariko Morimoto
et al.
Abstract:Process development to improve synthetic access to a potent, selective, and brain-penetrant tricyclic diazepine clinical candidate that inhibits mutant IDH1 is described. A variety of disconnections were evaluated to determine the preferred sequence of fragment coupling. The optimized route involves a metal-catalyzed C−N coupling/reductive cascade to form the central diazepine core, improved entries to both the zigzag morpholine and cyclohexyl acid peripheral pieces, and an efficient end-game sequence of acyla… Show more
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