Urea synthesis

To a solution of the amine compound (40mg, 0.082mmol) in pyridine (1mL) were added DMAP (50mg, 0.41 mmol), and diethylcarbamoyl chloride (0.103μl, 0.82mmol). The reaction mixture was stirred in a microwave oven at 120°C for 2h then cooled to RT over 16h. The reaction was diluted by adding 5% citric acid solution (10mL) and extracted with EtOAc (3 x 10mL). The combined organic extracts were washed with 5% citric acid solution (10mL), sodium hydrogen carbonate solution (10ml) and brine (10ml), dried over sodium sulphate, filtered and concentrated in vacuo to give the crude residue which was purified by AP3 (rf 2.68) to obtain the title compound (15mg = 31 % yield). 

 

Patent reference: WO2010015972 (Pfizer)

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