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

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Reaction Steps

The title compound was synthesized using an analogous procedure to that described in connection with Compound 3 except that 2-fluoro-beta-alaninate 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 1.55-1.87 (m, 11H) 1.91-2.08 (m, 3H) 2.18 (s, 3H) 2.79 (d, J=11.4 Hz, 2H) 3.24 (s, 3H) 3.61-3.83 (m, 3H) 3.94 (s, 3H) 4.77 (quin., J=8.3 Hz, 1H) 5.52 (qd, 1H) 7.47 (dd, J=1.8 Hz, 1H) 7.49 (s, 1H) 7.86 (s, 1H) 8.11 (d, J=7.8 Hz, 1H) 8.16 (s, 1H) 8.33 (d, J=8.34 Hz, 1H). [M+H] calc'd for C27H36FN7O3 526. found 526.

Provenance & Evidence