反应详情

The title compound was synthesized from 4-(9-cyclohexyl-7,7-difluoro-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-N-cyclopentyl piperazine-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 1.11-1.92 (m, 18 H) 2.93 (br. s., 4 H) 3.31 (s, 3 H) 3.93 (s, 3 H) 4.06 (t, J=13.39 Hz, 2 H) 4.44 (m, 1 H) 7.41 (d, J=8.0 Hz, 1 H) 7.43 (s, 1 H) 7.90 (s, 1 H) 8.21 (s, 1 H) 8.27 (d, J=8.34 Hz, 1 H) 9.37 (s, 1 H). Melting point: 98-99° C. [M+H] calculated for C31H42F2N8O3, 613; found 613.

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