Hydrochloric Acid → Tolvaptan

Participants

Reaction Steps

7-chloro-1-[2-methyl-4-(2-methyl benzoyl amino) benzoyl]-5 oxo-2,3,4,5-tetrahydro-1H-1-benzazepine (6.5 gm.) was suspended in methanol (104 ml) & water (10.4 ml) and then added sodium borohydride (0.385 gm.) at 30° C. and the reaction mixture was stirred for 1 hr. To the reaction mixture was added hydrochloric acid (39 ml). Then the reaction mixture was stirred for 2 hours. The solid obtained was collected by filtration and dried to give 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methyl benzoyl amino) benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine (5.8 gm.).

Provenance & Evidence