反应详情

2-Fluoro-5-(4-difluoromethoxybenzyl)oxybenzyl cis-2,6-dimethylpiperazine-1-carboxylate hydrochloride was prepared from 2-fluoro-5-hydroxybenzyl alcohol, 4-difluoromethoxybenzyl chloride and 1-chlorocarbonyl-2,6-dimethyl-4-tert-butoxycarbonylpiperazine according to the methods described for Examples 52 and 54 to give the product as a white solid (0.224 g, 94% overall); (Found: C, 55.7; H, 5.7; N, 5.9. C22H25F3N2O4.HCl requires C, 55.6; H, 5.5; N, 5.9%); δH (400 MHz, DMSO-d6) 9.8 (1H, br), 9.3 (1H, br), 7.50 (2H, d, J 8.4 Hz), 7.26(1H, t, J 74 Hz), 7.21–7.15 (3H, m), 7.09 (1H, m), 7.03 (1H, m, J 3.2 Hz), 5.12 (2H, s), 5.08 (2H, s), 4.28 (2H, m, J 6 Hz), 3.15 (2H, d, J 13 Hz), 3.06 (2H, dd, J 5 and 13 Hz), and 1.29 (6H, d, J 7.2 Hz).