反应详情

To a suspension of 2-[3-methoxy-4-(4-methyl-imidazol-1-yl)-phenylamino]-thiazole-4-carboxylic acid (61.5 mg, purity 43%, 0.080 mmol) in dichloromethane (2 ml) were added 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (24.5 mg, 0.128 mmol), 1-hydroxybenzotriazole hydrate (19.6 mg, 0.128 mmol), triethylamine (30.0 mg, 0.296 mmol) and a solution of 4-fluorobenzyl amine (12 mg, 0.096 mmol) in dichloromethane (1 ml). After 12 h at rt again 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (24.5 mg, 0.128 mmol), 1-hydroxybenzotriazole hydrate (19.6 mg, 0.128 mmol), triethylamine (30.0 mg, 0.296 mmol) and a solution of 4-fluorobenzyl amine (12 mg, 0.096 mmol) in dichloromethane (1 ml) were added. After 12 h at rt the reaction mixture was directly purified by silica gel chromatography using dichloromethane/methanol as eluent. The title compound was obtained as a off-white foam (23.0 mg, 66%). MS ISP (m/e): 438.2 (14) [(M+H)+].

1. customAfter 12 h at rt the reaction mixture was directly purified by silica gel chromatography