反应详情

The title compound was prepared according to the procedure for Example 102 using diethyl (4-{[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-ethoxybenzyl)phosphonate (Compound 244A 123.2 mg, 0.26 mmol) and ethyl cis-4-(7-amino-2-methyl-1-oxo-2,3-dihydro-1H-isoindol-4-yl)cyclohexanecarboxylate (100.0 mg, 0.32 mmol). The reaction mixture was concentrated in vacuo and purified by on an ISCO CombiFlash®Rf System eluting with: 0→5% MeOH in DCM] to afford 143.3 mg (73%) of the desired product. 1H NMR (400 MHz, MeOD) δ ppm 8.44 (d, J=10.36 Hz, 1H), 8.35 (s, 1H), 7.89 (d, J=8.34 Hz, 1H), 7.24 (d, J=8.59 Hz, 1H), 7.06 (t, J=2.15 Hz, 1H), 6.92 (dt, J=8.21, 2.21 Hz, 1H), 4.52 (s, 2H), 4.26 (q, J=7.16 Hz, 2H), 4.05-4.19 (m, 6H), 3.29 (s, 2H), 3.19 (s, 3H), 2.79 (br. s., 1H), 2.63-2.73 (m, 1H), 2.30 (d, J=7.33 Hz, 2H), 1.76 (d, J=6.06 Hz, 6H), 1.42 (t, J=6.95 Hz, 3H), 1.27-1.38 (m, 9H). MS (ES+): m/z 749.30/750.31 (100/25) [MH+] HPLC: tR=1.82 min (Micromass TOF: polar—3 min).

1. customThe title compound was prepared
2. concentrationThe reaction mixture was concentrated in vacuo
3. custompurified by on an ISCO CombiFlash®Rf System
4. washeluting with: 0→5% MeOH in DCM]