331947-66-1

Basic information

• Product Name: (R)-(+)-Tolvaptan
• Synonyms: (R)-(+)-Tolvaptan
• CAS NO: 331947-66-1
• Molecular Formula: C₂₆H₂₅ClN₂O₃
• Molecular Weight: 448.9413
• Product Categories: Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals
• Mol File: 331947-66-1.mol

Chemical Properties

• Appearance: /
• Storage Temp.: Refrigerator
• Solubility: Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
• CAS DataBase Reference: (R)-(+)-Tolvaptan(CAS DataBase Reference)
• NIST Chemistry Reference: (R)-(+)-Tolvaptan(331947-66-1)
• EPA Substance Registry System: (R)-(+)-Tolvaptan(331947-66-1)

Safety Data

• Hazardous Substances Data: 331947-66-1(Hazardous Substances Data)

Upstream product

• 137973-76-3 MOP-21826 
• 331947-59-2 (R)-7-chloro-5-methoxymethyloxy-1-(p-toluenesulfonyl)-2,3,4,5-tetrahydro-1H-1-benzazepine 
• 193686-74-7 (R)-5-acetoxy-7-chloro-1-(p-toluenesulfonyl)-2,3,4,5-tetrahydro-1H-1-benzazepine 
• 137982-91-3 7-chloro-1-(2-methyl-4-nitrobenzoyl)-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine 
• 193686-75-8 (R)-7-chloro-5-hydroxy-1-(p-toluenesulfonyl)-2,3,4,5-tetrahydro-1H-1-benzazepine 
• 331947-60-5 (R)-7-chloro-5-methoxymethyloxy-2,3,4,5-tetrahydro-1H-1-benzazepine 
• 331947-63-8 (R)-7-chloro-5-methoxymethyloxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine 

Relevant articles and documents

Method for preparing high-purity tolvaptan intermediate

The invention provides a method for preparing a high-purity tolvaptan intermediate, and concretely provides a method for purifying a tolvaptan intermediate N-[4-[(7-chloro-2,3,4,5-tetrahydro-5-oxo-1H-1-benzazepine-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide (formula II). A crude product containing the compound of formula II is recrystallized by an organic solvent composed of ester, haloalkaneand ether to preferably obtain the compound of formula II, having a purity of above 99.00%.

Efficient and promising asymmetric preparation of enantiopure tolvaptan via transfer hydrogenation with robust catalysts

Enantiopure tolvaptan, the first and only oral vasopressin antagonist for hyponatremia has been prepared by using an asymmetric transfer hydrogenation as a key step with HCOOH-Et3N or HCOONa-H2O as the hydrogen donor in open air. Good chemical yields with up to 99% enantioselectivity were obtained with a 1000:1 of S/C in an HCOONa-H2O system. The air and water stable catalysts provide a very promising prospect for industrial application.

Practical synthesis of both enantiomers of vasopressin V2 receptor antagonist OPC-41061 using the catalytic asymmetric hydrogenation

The optically active enantiomers of 7-chloro-5-hydroxy-1-[2methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5- tetrahydro-1H-1-benzazepine (OPC-41061, 1) were enantioselectively synthesized. The asymmetric transfer hydrogenation of the ketone (2), which is t

An efficient synthesis of optical isomers of vasopressin V2 receptor antagonist OPC-41061 by lipase-catalyzed enantioselective transesterification

The optically active enantiomers of 7-chloro-5-hydroxy-1-[2- methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro- 1H- 1-benzazepine (OPC-41061, 1) were enantioselectively synthesized. The chiral acetate ((R)-(-)-3) and the chiral alcohol ((S)-(+)-2) were prepared via the resolution of the racemic alcohol ((±)-2) using the lipase-mediated transesterification with vinyl acetate. Compounds ((R)-(-)-3) and ((S)-(+)-2) were converted to optically active 1.