反应详情

(R)-2-Methyl-piperazine-1-carboxylic acid 2,6-difluoro-4-(5-thiophen-2-yl-[1,2,4]oxadiazol-3-ylmethoxy)-benzyl ester was prepared from 2,6-difluoro-4-hydroxybenzyl alcohol, 3-chloromethyl-5-thiophen-2-yl-[1,2,4]oxadiazole and (R) 2-methylpiperazine resin according to the methods described for Example 126 to give the product as a yellow oil: δH(400 MHz; d6-DMSO) 1.10 (3H, d, J 7.0 Hz), 2.40 (1H, td, J 12.0, 3.5 Hz), 2.62 (2H, br d, J, 2.5 Hz), 2.75–2.82 (1H, br d, J 12 Hz), 2.88 (1H, td, J 12.5, 3.5 Hz), 3.55 (1H, br d, J 12 Hz), 3.96 (1H, br s), 5.02 (1H, d, J 12.5 Hz), 5.07 (1H, d, J 12.5 Hz), 5.42 (2H, s), 6.93–7.01 (2H, m), 7.36(1H, dd, J 5.0 and 4 Hz), 8.06 (1H, dd, J4, 1.0 Hz) and 8.12 (1H, dd, J 5.0, 1 Hz); HPLC (XTERRA, 50–80%, 235 nm) 99.8% (4.22 min).