反应详情

The title compound was synthesized from 4-(9-cyclopentyl-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=7.3 Hz, 3 H) 1.60-1.75 (m, 11 H) 1.84-2.09 (m, 5 H) 2.19 (s, 3 H) 2.80 (d, J=11.1 Hz, 2 H) 3.26 (s, 3 H) 3.60-3.83 (m, 3 H) 3.94 (s, 3 H) 4.78 (t, J=8.1 Hz, 1 H) 7.35-7.60 (m, 2 H) 7.80 (s, 1 H) 8.08 (d, J=7.6 Hz, 1 H) 8.16 (s, 1 H) 8.32 (d, J=8.3 Hz, 1 H). Melting point: 149-153° C. [M+H] calc'd for C29H40FN7O3, 554; found 554.

1. customas described in the General procedure for amide bond synthesis
2. customThe final compound was purified by reverse phase HPLC
3. customto give the free base