Ro3280 → 4-(9-cyclopentyl-7-fluoro-5-methyl-6-oxo-7-(trifluoromethyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide

Participants

Reaction Steps

The title compound was synthesized using the analogous procedure to that described in connection with Compound 3 except that 2-(aminomethyl)-2,3,3,3-tetrafluoropropanoic acid was used as the starting material. The final product was purified on reversed phase HPLC as TFA salt. 1H NMR (400 MHz, DMSO-d6) δ ppm 1.46-1.76 (m, 10H) 1.83-2.09 (m, 4H) 2.19 (s, 3H) 2.80 (d, J=11.9 Hz, 2H) 3.32 (s, 3H) 3.69-3.81 (m, 1H) 3.89 (t, 1H) 3.94 (s, 3H) 4.15-4.35 (q, 1H) 4.72 (quin., J=8.1 Hz, 1H) 7.48 (dd, J=1.77 Hz, 1H) 7.50 (s, 1H) 8.00 (s, 1H) 8.10 (d, J=7.8 Hz, 1H) 8.26 (d, J=8.3 Hz, 1H) 8.32 (s, 1H). [M+H] calc'd for C28H35F4N7O3 594. found 594.

Provenance & Evidence