Back to results
US 2014/0275523 A1Published application
Process for making benzoxazepin compounds
AssigneeGenentech, Inc.
InventorsRemy Angelaud, Danial R. Beaudry, Diane E. Carrera, Sushant Malhotra, Travis Remarchuk, Frederic St-Jean
Life of this patent
Estimating the term…
Abstract
Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula I, having the structure: and intermediates useful for the preparation of I.
Claims10
A process for preparing (2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide I, having the structure:
- and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, comprising:
- (a) reacting IV and 4,4,4′,4′,5,5,5′,5′-octamethyl-2,2′-bi(1,3,2-dioxaborolane) to form 22
- (b) reacting 22, a palladium catalyst, and III to form 23
- (c) reacting 23 with an aqueous basic reagent to form II
- and
- (d) reacting II with an acyl activating reagent, followed by ammonia to give I.
3 more elements
A compound selected from the structures:
Dependencies are inferred from the claim text.