2-[4-(difluoromethoxy)-3-methoxyphenyl]acetonitrile synthesis

Yield:852851-91-3 98%

Reaction Conditions:

in dimethyl sulfoxide at 20; for 7 h;

Steps:

To a solution of intermediate 63 (0.15 g, 0.69 mmol) in dimethylsulfoxide (1.6 mL) was added sodium cyanide (40 mg, 0.82 mmol). The mixture was stirred at room temperature for 7 hours. The reaction was poured into water (10 mL) and extracted with ethyl acetate (2x5 mL). The organic layer was washed with brine (2x5 mL), dried (Na2SO4), and the solvent removed under reduced pressure. The title compound was obtained (144 mg, 98%). 8 (250 MHz, CDCI3) : 3.71 (s, 2H); 3.84 (s, 3H); 6.53 (t, JF-H=75. 0 Hz, 1 H) ; 6. 83 (s, 1 H) ; 6.88 (dd, J1=2. 0 Hz, J2=8. 0 Hz, 1 H) ; 7.10 (d, J=8.0 Hz, 1 H).

References:

WO2005/58883,2005,A1 Location in patent:Page/Page column 132