Process for the preparation of a benzazepine derivative

摘要

Provided is an industrially scalable process for the preparation of a benzazepine derivative, namely, 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methyl benzoyl amino) benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine (generically referred as Tolvaptan).

主权项

1. A process for the preparation of Tolvaptan comprising reducing (7-chloro-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-5-oxo-2,3,4,5-tetrahydro-1H-1benzazepine) of Formula 2using a hydrogenating agent selected from the group comprising of lithium borohydride, sodium borohydride, zinc borohydride, and potassium borohydride in a solvent mixture comprising an alcohol selected from the group comprising of methanol, ethanol, n-propanol, isopropanol and t-butanol and water, wherein the percentage of water in the solvent mixture is 5% to 30%.