反应详情

750 mg 3-cyanomethyl-8-hydroxy-2-methyl-imidazo[1,2-a]pyridine are reacted, analogously to the method described in Example 21, with 210 mg (-)-1R,2S-indenoxide and 400 mg triethylamine in aqueous methanol (60 ml methanol+15 ml water) at room temperature. After 3 days the solution is evaporated and the residue taken up in 50 ml water. The precipitate is filtered off and purified by chromatography over silica gel (mobile phase: ethyl acetate/methanol=10:1). After evaporation the residue is precipitated from methylene chloride/cyclohexane. 120 mg of the title compound is isolated. [α]D22 =+113° (c=1, chloroform).

1. customAfter 3 days the solution is evaporated
2. filtrationThe precipitate is filtered off
3. custompurified by chromatography over silica gel (mobile phase: ethyl acetate/methanol=10:1)
4. customAfter evaporation the residue
5. customis precipitated from methylene chloride/cyclohexane