反应详情

Dimethyl 13-cyclohexyl-6,7-dihydro-5H-indolo[1,2-d][1,4]benzodiazepine-6,10-dicarboxylate was dissolved in anhydrous MeOH (0.05M) and HOAc was added. the mixture was treated with a 37% solution of formaldehyde in water (1.2 eq.), then NaCNBH3 (1.2 eq.) was added. The solution was stirred for 2 h at RT. The product was isolated by flash chromatography (PE:EtOAc, 9:1, 0.5% NEt3). After evaporation of the solvents a colourless solid was obtained (quant.). (ES+) m/z 447 (M+H)+.

1. customAfter evaporation of the solvents a colourless solid
2. customwas obtained (quant.)