4-Amino-1-methylpiperidine → 4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-N-(1-methyl-piperidin-4-yl)-3-trifluoromethyl-benzamide

関与物質

反応手順

The title compound was synthesized from 4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-(trifluoromethyl)benzoic 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, CHLOROFORM-d) δ ppm 1.34-1.67 (m, 9H) 1.70-1.85 (m, 3H) 2.13 (br. s., 1H) 2.27 (s, 3H) 2.84-2.93 (m, 1H) 3.32 (s, 3H) 3.74-3.86 (m, 1H) 4.00 (t, J=14.0 Hz, 1H) 4.50 (quin, 1H) 7.96 (d, J=8.6 Hz, 1H) 8.12 (dd, 1H) 8.20 (s, 1H) 8.21 (s, 1H) 8.48 (d, J=7.8 Hz, 1H) 8.52 (s, 1H). [M+H] calc'd for C27H32F5N7O2, 582. found 582.

情報源と証拠