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US 10,851,070 B2Granted
Processes for the resolution of benzodiazepin-2-one and benzoazepin-2-one derivatives
AssigneeEnata Pharmaceuticals, Inc.
InventorsAndrew Hague, Matthew Ronsheim
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Abstract
The present invention relates to processes and intermediates useful in the preparation of biologically active molecules, especially in the synthesis of Respiratory Syncytial Virus (RSV) inhibitors. The present invention also relates to processes and intermediates for the preparation of compounds of Formula (I-0) and Formula (I):
Claims15
A process for the preparation of a compound of Formula (I-0):
- wherein X is N;
- R1 is halogen, CN or optionally substituted C1-C3 alkyl;
- and n is 0, 1, 2 or 3;
- said process comprising:
- (a) reacting a compound of Formula (I′-0),
- with a compound of Formula (III),
- wherein R is optionally substituted phenyl, in a solvent selected from acetonitrile, methanol, tetrahydrofuran, 2-methyltetrahydrofuran, ethyl acetate, 1,2-dimethoxyethane, dichloromethane, 1,4-dioxane, toluene, anisole, ethanol, acetone, N,N-dimethylformamide, N,N-dimethylacetamide, pyridine and isopropyl acetate, or a combination of two or more thereof and at a temperature of 20° C. to 45° C., to yield a compound of Formula (IV-0),
- provided that said reaction takes place in the absence of an aromatic aldehyde;
- and
- (b) treating the compound of Formula (IV-0) with a base to provide the compound of Formula (I-0).
7 more elements
Dependencies are inferred from the claim text.