反应详情

1-({2-(Hex-5-enyl-methyl-carbamoyl)-4-[2-(4-isopropyl-thiazol-2-yl)-7-methoxy-quinolin-4-yloxy]-cyclopentanecarbonyl}-amino)-2-vinyl-cyclopropanecarboxylic acid ethyl ester (33, 280 mg) was dissolved in DCE (280 mL) in a reflux setup. The system was successively evacuated and filled with argon (repeated 3 times). Then, Hoveyda-Grubbs 2nd generation catalyst (28 mg) was added and the system was evacuated and filled with argon twice. The resulting mixture was successively heated to refluxed overnight, concentrated, and subjected to flash column chromatography (silica, AcOEt/hexane) to give 197 mg (73%) of the title product 34 as grey-brown solid: m/z=661 (M+H)+.

1. customThe system was successively evacuated
2. additionfilled with argon (repeated 3 times)
3. additionThen, Hoveyda-Grubbs 2nd generation catalyst (28 mg) was added
4. customthe system was evacuated
5. additionfilled with argon twice
6. temperatureThe resulting mixture was successively heated
7. temperatureto refluxed overnight
8. concentrationconcentrated