abstract |
【Task】 Optically active N-[(S) -1-hydroxypropane-2-yl] -4-methyl-1- [2-methyl-4- (3-methyl-1H-pyrazole-1-yl) benzoyl] -2 , 3,4,5-Tetrahydro-1H-benzo [b] Azepine-4-carboxamide can be efficiently produced by providing a novel production method. SOLUTION: 1- (2-Methyl-4- (3-Methyl-1H-pyrazole-1-yl) benzoyl) -5-oxo-2,3,4,5-tetrahydro-1H-benzo [b] azepine-4-carboxylic acid Ethyl acid acid is methylated in an organic solvent in the presence of a specific asymmetric quaternary ammonium salt and a base with a methylating agent to (R) -4-methyl-1- (2-methyl-4- (3). -Methyl-1H-pyrazole-1-yl) benzoyl) -5-oxo-2,3,4,5-tetrahydro-1H-benzo [b] Azepine-4-carboxylic acid ethyl ester. [Selection diagram] None |