Triethylamine → (+/-)-4-Chloro-2-methoxy-N-(4-oxo-2-pyrimidin-4-yl-5,6,8,9-tetrahydro-4H-7-oxa-1,4a-diaza-benzocyclohepten-9-yl)benzamide

Participants

Reaction Steps

To a solution of 0.700 g (2.70 mmol) of (+/−)-9-amino-2-pyrimidin-4-yl-5,6,8,9-tetrahydro-7-oxa-1,4a-diaza-benzocyclohepten-4-one dissolved in 54 mL of dimethylformamide was added 0.554 g (2.97 mmol) of 4-chloro-2-methoxy-benzoic acid. To the resulting mixture was added 440 μL (2.97 mmol) of diethyl cyanophosphonate and 450 μL (3.24 mmol) of triethylamine at 0° C. The resulting mixture was stirred at room temperature for 4 hours. Water and ethyl acetate were added and the mixture was stirred. The resulting residue was filtered, washed with water, ethyl acetate and diethyl ether to afford 0.932 g (81%) of the pure product as a white powder.

Provenance & Evidence