反应详情

The title compound was synthesized in two steps. The first as described for Intermediate example I-97, starting from 5-(methoxycarbonyl)pyridine-2-carboxylic acid and 4,4-difluorocyclohexylamine hydrochlorid, and the second as described for Intermediate example I-98 at 55° C., starting from the product received in the first step which was first purified by column chromatography using a gradient of ethyl acetate in heptane. Total yield (two steps) 65%; 1H NMR (400 MHz, DMSO-d6) δ ppm 9.08 (dd, 1 H), 8.89 (d, 1 H), 8.43 (dd, 1 H), 8.13 (dd, 1 H), 3.95-4.07 (m, 1 H), 1.68-2.11 (m, 8 H); MS (ESI) m/z 285[M+H+], m/z 283[M−H+];

1. customat 55° C.
2. customwas first purified by column chromatography
3. customTotal yield (two steps) 65%