Acetic Acid → HCID 12146683, compound

Participants

Reaction Steps

2-(3-Aminophenyl)-4-phenyl-4H-1,3,4-oxadiazine-5(6H)-one (200 mg) obtained in Example 78 was dissolved in acetonitrile (5 ml), and 37% aqueous formaldehyde (1 ml) and sodium cyanoborohydride (250 mg) were added thereto, and acetic acid (0.15 ml) was added dropwise thereto over 5 minute, and mixed at room temperature for 6 hours. The reaction solution was diluted with ethyl acetate, washed with an aqueous saturated sodium bicarbonate and brine, and dried over anhydrous magnesium sulfate. After the drying agent was filtered off, the filtrate was evaporated and purified by silica gel chromatography (hexane/ethyl acetate system), to give the title compound (215 mg, 97%).

Provenance & Evidence