反应详情

To a solution of N,N′-di-tert-butoxycarbonyl-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-2-carboxamidine (50 mg) and 4-bromomethylpiperidine-1-carboxylic acid benzyl ester (120 mg) in dimethyl sulfoxide (1 ml) was added 4N aqueous sodium hydroxide solution (0.13 ml), and the mixture was stirred at room temperature for 17 hours. After completion of the reaction, water was added, and the mixture was extracted with ethyl acetate and washed successively with water and saturated brine. The organic layer was dried over anhydrous sodium sulfate, and the solvent was evaporated. The obtained residue was purified by silica gel column chromatography (hexane:acetone=5:1) and dried under reduced pressure to give the title compound (55 mg).

1. additionwas added
2. extractionthe mixture was extracted with ethyl acetate
3. washwashed successively with water and saturated brine
4. dry with materialThe organic layer was dried over anhydrous sodium sulfate
5. customthe solvent was evaporated
6. customThe obtained residue was purified by silica gel column chromatography (hexane:acetone=5:1)
7. customdried under reduced pressure