4-Amino-1-methylpiperidine → 4-(9-Cyclohexyl-7-ethyl-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

Participants

Reaction Steps

The title compound was synthesized from 4-(9-cyclohexyl-7-ethyl-7-fluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[5,4-b][1,4]diazepin-2-ylamino)-3-methoxybenzoic acid as described in the General procedure for amide bond synthesis using HATU and. 1-methylpiperidin-4-amine. The final compound was purified by reverse phase HPLC and basified to give the free base. 1H NMR (400 MHz, DMSO-d6) δ ppm 0.89 (t, J=7.4 Hz, 3 H) 1.08-2.06 (m, 16 H) 2.20 (s, 3 H) 2.82 (d, J=11.1 Hz, 2 H) 3.25 (s, 4 H) 3.60-3.85 (m, 3 H) 3.95 (s, 3 H) 4.49 (m, 1 H) 7.47 (d, J=8.3 Hz, 1 H) 7.50 (s, 1 H) 7.77 (s, 1 H) 8.01-8.19 (m, 2 H) 8.31 (d, J=8.3 Hz, 1 H). [M+H] calc'd for C30H42FN7O3, 568; found 568.

Provenance & Evidence