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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1486488Generated: November 1, 2026

Water → Tolvaptan

https://huagongshe.com/reaction/1486488

Reaction equation

Participants

RoleNameHCIDCharge
ReactantWaterHCID 962—
ReactantSodium borohydrideHCID 4311764—
Reactant5-Dehydro TolvaptanHCID 11362843—
SolventMethanolHCID 887—
ProductTolvaptanHCID 21623785%

Reaction Conditions

Temperature27.5 °C

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 methanol (48 ml) & water (12 ml) and then added sodium borohydride (0.236 gm.) at 25° C. and the reaction mixture was stirred for 1hr. To the reaction mixture was added water (12 ml) and stirred for 2 hours at 25-30° C. The solid obtained was collected by filtration and dried to give 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino) benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine (1.70 gm).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09428461B2
Source datasetuspto-grants-2016_08
ORD IDord-b17d24d71c064db9b9220bc520c52eeb
Source noteuspto-grants-2016_08