反应详情

2 g of ethyl mono (4-methylbenzenesulfonate) aminocyano acetate of Stage B of Example 1 and 1.9 g of N-[(dimethylamino) methylene]-4'-formyl-(1,1'-biphenyl)-2-sulfonamide of Stage A of Example 1 were stirred in dichloromethane at 35° for 3 hours and then 0.396 g of sodium cyano borohydride were added. The solution was stirred at ambient temperature for 18 hours and the reaction mixture was filtered, washed with water and evaporated. After chromatography on silica (dichloromethane-ethyl acetate 85-15), 770 mg of the expected product were obtained, identical to that of Stage C of Example 1.

1. filtrationthe reaction mixture was filtered
2. washwashed with water
3. customevaporated