反应详情

A solution of 3.24 g of (R)-2-(tetrazolo-[1,5-a]pyrid-6-yl)oxirane and 5.89 g of 1-methyl-2-(5-benzyloxy-1H-indol-3-yl)ethyl amine in 84 ml of absolute ethanol was heated at reflux under nitrogen for 24 hours. The reaction mixture was concentrated and the residue purified by preparative TLC on silica gel (95:5:0.5 CH2Cl2 :MeOH:NH4OH) to give 1.29 g of (R)-α-[[(1(R)-methyl-2-(5-benzyloxy-1H-indol-3-yl)ethyl)amino]methyl]tetrazolo[1,5-a]pyridine-6-methanol and 1.46 g of (R)-α-[[(1(S)-methyl-2-(5-benzyloxy-1H-indol-3-yl)ethyl)-amino]methyl]tetrazolo[1,5-a]pyridine-6-methanol.

1. temperatureat reflux under nitrogen for 24 hours
2. concentrationThe reaction mixture was concentrated
3. customthe residue purified by preparative TLC on silica gel (95:5:0.5 CH2Cl2 :MeOH:NH4OH)