反应详情

Use a method similar to the General Procedure 1-4 to deprotect 3-tert-butoxy carbonyl-7-chloro-6-(3-fluoro-4-propylcarbamoyl-benzylamino)-2,3,4,5-tetrahydro-1H-benzo[d]azepine (33.1 mg, 0.83 mmol) in 1,4-dioxane (1 mL). Purify by SCX chromatography eluting with dichloromethane and dichloromethane/2M ammonia in methanol (1:1) to afford 7-chloro-6-(3-fluoro-4-propylcarbamoyl-benzylamino)-2,3,4,5-tetrahydro-1H-benzo[d]azepine as a colorless oil (25.2 mg, 96%). MS (ES+) m/z: 390.1 (M+H)+. Use a method similar to the General Procedure 2-6, using 7-chloro-6-(3-fluoro-4-propylcarbamoyl-benzylamino)-2,3,4,5-tetrahydro-1H-benzo[d]azepine (25 mg, 0.064 mmol) to provide the title compound as a white foam (31.4 mg, 91%). MS (ES+) m/z: 390.1 (M+H)+.

1. customPurify by SCX chromatography
2. washeluting with dichloromethane and dichloromethane/2M ammonia in methanol (1:1)