反应详情

To a solution of N,N′-di-tert-butoxycarbonyl-7-(piperidin-4-ylmethoxy)-1,2,3,4-tetrahydroisoquinoline-2-carboxamidine (120 mg) in a mixture of tetrahydrofuran (1.2 ml) and dimethylformamide (1.2 ml) were added triethylamine (0.068 ml) and 2-chloro-5-nitropyridine (58 mg), and the mixture was stirred at room temperature for 2 hours. After completion of the reaction, 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=4:1) and dried under reduced pressure to give the title compound (120 mg).

1. customAfter completion of the reaction
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=4:1)
7. customdried under reduced pressure