3-(Chloromethyl)-5-(thiophen-2-yl)-1,2,4-oxadiazole → HCID 69141856, Verbindung

Beteiligte Stoffe

Reaktionsschritte

cis-2,6-Dimethyl-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 cis-1-chlorocarbonyl-2,6-dimethyl-4-tert-butoxycarbonylpiperazine according to the methods described for Example 54 and 121 to give the product as a yellow oil: δH(400 MHz; d6-DMSO) 1.14 (6H, d, J 6.5 Hz), 2.60 (2H, dd, J 12, 5 Hz), 2.66 (2H, d, J 12 Hz), 3.77–3.87 (2H, m), 5.05 (2H, s), 5.42 (2H, s), 6.93–7.01 (2H, m), 7.36 (1H, dd, J 5.0, 4 Hz), 8.06 (1H, dd, J 4, 1.0 Hz) and 8.12 (1H, dd, J 5.0, 1.0 Hz); HPLC (XTERRA, 50–80%, 235 nm) 99.4% (5.04 min).

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