331947-69-4

Upstream product

• 317374-08-6 2-methyl-4-(2-methylbenzoylamino)benzoic acid 

Downstream Products

• 926035-31-6 (4S,5S)-4,5-bis(methoxymethoxy)-7-chloro-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine 
• 926035-32-7 (4S,5R)-4,5-bis(methoxymethoxy)-7-chloro-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine 
• 926035-33-8 (4R,5S)-4,5-bis(methoxymethoxy)-7-chloro-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine 
• 137973-76-3 MOP-21826 
• 150683-30-0 tolvaptan 
• 1296212-28-6 N-(4-(7-chloro-2,3-dihydro-5-oxo-2,2,4,4-tetradeutero-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide 
• 1296212-20-8 N-(4-(7-chloro-2,3-dihydro-5-hydroxy-2,2,4,4,5-pentadeutero-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide 
• 1296212-27-5 N-(4-(7-chloro-5-oxo-2,2-dideutero-3,4-dihydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide 
• 1296212-19-5 N-(4-(7-chloro-5-hydroxy-2,2-dideutero-3,4,5-trihydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide 
• 1296212-26-4 N-(4-(5-(tert-butyldimethylsilyloxy)-7-chloro-2,2-dideutero-3,4,5-trihydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide 
• 331947-63-8 (R)-7-chloro-5-methoxymethyloxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine 
• 331947-57-0 (S)-7-chloro-5-methoxymethyloxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine 

Relevant academic research and scientific papers

Efficient synthesis of optically active 4,5-dihydroxy-2,3,4,5-tetrahydro-IH-1-benzazepine derivatives utilizing lipase-catalyzed transesterification

As an efficient and enantioselective synthesis of the 4,5-dihydroxybenzazepine compounds, the syntheses of optically active 5-0-protected tranAs an efficient and enantioselective synthesis of the 4,5-dihydroxybenzazepine compounds, the syntheses of optica

Preparation method of high-purity tolvaptan

The invention provides a preparation method of high-purity tolvaptan. Specifically, the quality of an intermediate N-(4-(7-chloro-5-oxo-2, 3, 4, 5-tetrahydro-1H-benzo[b]aza-1-ylcarbonyl)-3-methylphenyl)-2-methylbenzamide is controlled through crystallization and purification, so that the high-purity intermediate is obtained, and the high-purity tolvaptan is obtained by controlling the process conditions of reducing the intermediate to obtain the tolvaptan and subsequently purifying the tolvaptan. The method is low in cost, simple in preparation process and mild in reaction condition, the purity of the prepared tolvaptan reaches 99.9% or above, the yield reaches 80% or above, and industrial production is facilitated.

MANUFACTURING METHOD OF TOLVAPTAN, SALT THEREOF AND SOLVATE

PROBLEM TO BE SOLVED: To provide a manufacturing method of high purity and high yield tolvaptan, a salt thereof, or a solvate thereof without using a solvent with large environmental load, and having enhanced operability of a reaction. SOLUTION: There is provided a manufacturing method of tolvaptan, a salt thereof, or a solvate thereof, including a process for reacting following a described carboxylic acid derivative (I) with a chlorination agent such as thionyl chloride to convert it to a corresponding acid chloride (I), in which the reaction process is conducted in a presence of a solvent having relative dielectric constant of 10 or more and donor number of 20 or more, and represented by N,N-dimethyl acetamide, N-methyl-2-pyrrolidone, N.N'-dimethyl propylene urea or N,N,N',N'-tetramethyl urea. SELECTED DRAWING: None COPYRIGHT: (C)2020,JPOandINPIT

BENZAZEPINE COMPOUND

An object of the present invention is to provide a novel benzazepine compound or a salt thereof, which has excellent vasopressin antagonistic activity. The benzazepine compound or a salt thereof of the present invention is represented by Formula (1): wher