反应详情

To a solution of 2-methyl-6-((2S,3′S)-2-methyl-[1,3′]bipyrrolidinyl-1′-yl)-pyridin-3-ylamine (0.025 g, 0.096 mmol) in dichloromethane (3 mL) and pyridine (0.5 mL) was added 1-naphthoyl chloride (0.055 g, 0.288 mmol). The reaction mixture was allowed to stir for 16 hours at room temperature. The reaction mixtures were filtered through a 2.0 g Varian Bond Elut SCX (stong cation-exchange) cartridge eluting with 20 mL of methanol, followed by 7N ammonia in methanol (20 mL), and concentrated under vacuum. The crude product was purified over a silica gel column eluting with methanol in dichloromethane (0-10%) over 30 minutes to obtain 0.0247 g (62%) of the compound.

1. customThe reaction mixtures
2. filtrationwere filtered through a 2.0 g Varian Bond Elut SCX (stong cation-exchange) cartridge
3. washeluting with 20 mL of methanol
4. concentrationconcentrated under vacuum
5. customThe crude product was purified over a silica gel column
6. washeluting with methanol in dichloromethane (0-10%) over 30 minutes