反应详情

2-[3-(3-Cyano-phenyl)-[1,2,4]oxadiazol-5-yl]-6-methyl-piperidine-1-carboxylic acid tert-butyl ester (340 mg, 46.2%) was prepared according to the procedure in Example 25 from 6-methyl-piperidine-1,2-dicarboxylic acid 1-tert-butyl ester (486 mg, 2 mmol) with isobutyl chloroformate (273.16 mg, 2.0 mmol) and triethylamine (1.14 g, 8 mmol) in THF (6 mL). Then 3-cyano-N-hydroxy-benzamidine (306 mg, 1.9 mmol) and DMF (5 mL) were added and the mixture was heated at 130˜135° C. for 3 h. 1H NMR (CDCl3), δ(ppm): 8.38 (d, 1H), 8.32 (dd, 1H), 7.77 (dd, 1H), 7.61 (t, 1H), 5.58 (d, 1H), 4.43 (m, 1H), 2.55 (m, 1H), 1.50–1.98 (m & s, 14H), 0.96 (d, 3H).

1. temperaturethe mixture was heated at 130˜135° C. for 3 h