反应详情

The title compound was synthesized from 4-(9-cyclohexyl-7-fluoro-7-vinyl-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 (R)-1-Boc-3-aminopiperidine. Further, after washing with water (10 ml), t-butoxycarbonyl (Boc) protection group was removed using 40% TFA in dichloromethane (6 ml) and purified the product using preparative HPLC. 1H NMR (400 MHz, DMSO-d6) δ ppm 1.41-2.00 (m, 12H) 2.39 (t, J=6.5 Hz, 2H) 2.81 (d, J=12.38 Hz, 1H) 2.96 (d, J=12.38 Hz, 1H) 3.28 (s, 3H) 3.70-3.88 (m, 3H) 3.94 (s, 2H) 4.88 (m, 1H) 5.37 (d, 2H) 6.00 (m, 1H) 7.47 (d, J=8.0 Hz, 1H), 7.48 (br. s., 1H) 7.82 (s, 1H) 7.98 (d, J=8.0 Hz, 1H) 8.12 (s, 1H) 8.30 (d, J=8.0 Hz, 1H). Melting point: 169-172° C. [M+H] calculated for C28H36FN7O3, 538. found 538.

1. customas described in the General procedure for amide bond synthesis
2. washFurther, after washing with water (10 ml), t-butoxycarbonyl (Boc) protection group
3. customwas removed
4. custompurified the product