反应详情

A mixture of (-)-3-methyl-2-[2-[[1-(5-methyl-1-trityl-1H-imidazol-4-yl)ethyl]amino]ethyl]indole (2.7 g), N,N'-carbonyldiimidazole (2.2 g), 1,8-diazabicyclo[5.4.0]-7-undecene (861 mg) and molecular sieves (810 mg) in dry tetrahydrofuran (40 ml) was stirred at reflux for 2 hours. The reaction mixture was diluted with ethyl acetate, washed with water and brine, dried over anhydrous magnesium sulfate and evaporated in vacuo. The residue was chromatographed over silica gel (eluted with 5% ethyl acetate in chloroform) to give (+)-3,4-dihydro-5-methyl-2-[1-(5-methyl-1-trityl-1H-imidazol-4-yl)ethyl]pyrimido[1,6-a]indol-1(2H)-one (2.09 g) as amorphous powder.

1. temperatureat reflux for 2 hours
2. washwashed with water and brine
3. dry with materialdried over anhydrous magnesium sulfate
4. customevaporated in vacuo
5. customThe residue was chromatographed over silica gel (eluted with 5% ethyl acetate in chloroform)