Methyl 1-(pyridin-2-ylmethyl)piperidine-2-carboxylate → 2-{2-[3-(3-Methoxy-phenyl)-[1,2,4]oxadiazol-5-yl]-piperidin-1-ylmethyl}-pyridine

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Reaktionsschritte

1-Pyridin-2-ylmethyl-piperidine-2-carboxylic acid methyl ester (50 mg, 0.213 mmol) was mixed with N-hydroxy-3-methoxy-benzamidine (29 mg, 0.174 mmol) and sodium tert-butoxide (19 mg, 0.20 mmol) in toluene (0.5 mL) in a sealed vial at 130° C. for 10 min. The reaction mixture was cooled down and diluted with dichloromethane, washed with water. The title compound was purified by silica gel colomn chromatography with 20˜30% ethyl acetate in hexanes to give a colorless oil, 20 mg (32.7%). 1H NMR (CDCl3), δ(ppm): 8.50 (d, 1H), 7.66 (m, 3H), 7.47 (d, 1H), 7.38 (t, 1H), 7.13 (dd, 1H), 7.03 (dd, 1H), 4.11 (t, 1H), 3.88 (s, 3H), 3.73 (dd, 2H), 3.04 (m, 1H), 2.42 (m, 1H), 2.03 (m, 2H), 1.46-1.90 (m, 4H).

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