反应详情

A mixture of 3.8 parts of 3-(2-chloroethyl)-2,8-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one, 3 parts of 3-(4-piperidinyl)-1H-indole, 10 parts of sodium carbonate, 0.1 parts of potassium iodide and 240 parts of 4-methyl-2-pentanone is stirred and refluxed for 20 hours. The reaction mixture is filtered hot over Hyflo and the filtrate is evaporated. The residue is purified by column-chromatography over silica gel using a mixture of trichloromethane and methanol (90:10 by volume) as eluent. The pure fractions are collected and the eluent is evaporated. The residue is crystallized from a mixture of 2-propanol, 2,2'-oxybispropane and 4-methyl-2-pentanone, yielding 4.7 parts of 3-[2-[4-(1H-indol-3-yl)-1-piperidinyl]ethyl]-2,8-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one; mp. 235.9° C.

1. temperaturerefluxed for 20 hours
2. filtrationThe reaction mixture is filtered hot over Hyflo
3. customthe filtrate is evaporated
4. customThe residue is purified by column-chromatography over silica gel using
5. additiona mixture of trichloromethane and methanol (90:10 by volume) as eluent
6. customThe pure fractions are collected
7. customthe eluent is evaporated
8. customThe residue is crystallized from a mixture of 2-propanol, 2,2'-oxybispropane and 4-methyl-2-pentanone