5-Dehydro Tolvaptan → Tolvaptan

HRID 1486484Notes

Reaction equation

HRID 1486484 reaction equation
[Cl:1][C:2]1[CH:3]=[CH:4][C:5]2[N:11]([C:12](=[O:30])[C:13]3[CH:18]=[CH:17][C:16]([NH:19][C:20](=[O:28])[C:21]4[CH:26]=[CH:25][CH:24]=[CH:23][C:22]=4[CH3:27])=[CH:15][C:14]=3[CH3:29])[CH2:10][CH2:9][CH2:8][C:7](=[O:31])[C:6]=2[CH:32]=1>O>[CH3:27][C:22]1[CH:23]=[CH:24][CH:25]=[CH:26][C:21]=1[C:20]([NH:19][C:16]1[CH:17]=[CH:18][C:13]([C:12]([N:11]2[C:5]3[CH:4]=[CH:3][C:2]([Cl:1])=[CH:32][C:6]=3[CH:7]([OH:31])[CH2:8][CH2:9][CH2:10]2)=[O:30])=[C:14]([CH3:29])[CH:15]=1)=[O:28]

Participants

3

Reactant 1

HCID 113628435-Dehydro Tolvaptan

Product 1

HCID 216237Tolvaptan

Reagents, catalysts & solvents 1

HCID 962WaterSolvent

Procedure

In a preferred embodiment of the present invention, starting material 7-chloro-1-[2-methyl-4-(2-methylbenzoylamino) benzoyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine of Formula 2 is reduced using hydrogenating agent in a solvent mixture containing alcohol and water to obtain Tolvaptan of Formula 1.

Sources & evidence

ORD record
ord-ad785b99425d449db216b668d33c6312
Source dataset
uspto-grants-2016_08
Patent number
US09428461B2

Reaction notes

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