反应详情

2-{5-[5-(4-Methoxy-phenyl)-pyrimidin-2-ylamino]-2-methyl-pyridin-3-ylcarbamoyl}-piperidine-1-carboxylic acid tert-butyl ester 20 is dissolved in DCM (1 mL) and TFA is added (2 mL). The yellow solution is stirred at rt for 2 h. The solvent and the excess of TFA are removed under vacuum and the residue is purified by preparative LCMS to afford piperidine-2-carboxylic acid {5-[5-(4-methoxy-phenyl)-pyrimidin-2-ylamino]-2-methyl-pyridin-3-yl}-amide C1. 1H NMR (400 MHz, d6-DMSO) δ 1H NMR (400 MHz, d4-CH3OH) δ 9.27 (d, J=4.0 Hz, 1H), 8.85 (d, J=4.0 Hz, 1H), 8.80 (s, 2H), 7.59-7.57 (m, 2H), 7.06-7.06 (m, 2H), 4.14 (dd, J=4.0 and 12.0 Hz, 1H), 3.86 (s, 3H), 3.52-3.48 (m, 1H), 3.15-3.12 (m, 1H), 2.62 (s, 3H), 2.45-2.44 (m, 1H), 2.07-2.06 (m, 1H), 1.98-1.95 (m, 1H), 1.89-1.85 (m, 1H), 1.79-1.75 (m, 2H). MS (m/z) (M+1)+: 419.2.

1. customThe solvent and the excess of TFA are removed under vacuum
2. customthe residue is purified by preparative LCMS