4-Aminobenzamide → 4-((4-(Benzyloxy)-5-iodopyrimidin-2-yl)amino)benzamide

Participants

Reaction Conditions

Reaction Steps

To a solution of 4-(benzyloxy)-2-chloro-5-iodopyrimidine (J1, 2.02 g) and 4-aminobenzamide (3.97 g) in N-methylpyrrolidone (20 mL), (1S)-(+)-10-camphorsulfonic acid (6.76 g) was added at room temperature, and the mixture was stirred at 60° C. for 9 hours. The reaction mixture was cooled on ice, and then poured into saturated aqueous sodium hydrogencarbonate. The solid matter was taken by filtration, washed with a mixed solvent of ethyl acetate and methanol, and then dried under reduced pressure to obtain 4-((4-(benzyloxy)-5-iodopyrimidin-2-yl)amino)benzamide (J10, 3.05 g) as white solid.

Provenance & Evidence