反应详情

2-[(Isoquinoline-3-carbonyl)-amino]-1H-benzoimidazole-5-carboxylic acid methyl ester was prepared from 1.9 g (10 mmol) of isoquinoline-3-carboxylic acid monohydrate, 4.6 g (12 mmol) of HBTU, and 1.9 g, (10 mmol) of 2-amino-1H-benzoimidazole-5-carboxylic acid methyl ester as described in general procedure A. A 0.35 g (1.0 mmol) portion of 2-[(isoquinoline-3-carbonyl)-amino]-1H-benzoimidazole-5-carboxylic acid methyl ester was subsequently hydrolyzed according to general procedure B to give 2-[(isoquinoline-3-carbonyl)-amino]-1H-benzoimidazole-5-carboxylic acid as a light yellow solid, which was used in the final coupling step without further purification.