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0 °C

To a solution of 2-cyano-5-(2-fluoro-4-trimethylsilanylphenylamino)-terephthalic acid dimethyl ester (300 mg, 0.75 mmol) in methanol (15 ml) and DCM (2 ml) at 0° C. was added silica (1 g) and cobalt (II) chloride hexahydrate (357 mg, 1.50 mmol) followed by sodium borohydride (285 mg, 7.50 mmol). During the addition of the sodium borohydride large amounts of effervescence were observed and the reaction turned black. The reaction mixture was stirred at 0° C. for 1 hour. The reaction was filtered and the filtrate concentrated in vacuo to provide a residu that was subjected to flash chromatography (SiO2, gradient 0-20% methanol in DCM) to yield the title compound as a brown solid (138 mg, 49%). LCMS (Method B): RT=4.18 min, 2M+H−=745 (100%), M+H+=373 (25%).

1. filtrationThe reaction was filtered
2. concentrationthe filtrate concentrated in vacuo
3. customto provide a residu that