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 (2 gm.) was suspended in n-propanol (80 ml) & water (12 ml) and then added sodium borohydride (0.253 gm.) at 35° C. and the reaction mixture was stirred for 1 hr. To the reaction mixture was added hydrochloric acid (12 ml). Than the reaction mixture was stirred for 1 hour. 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 (1.65 gm).

Provenance & Evidence