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Triphenylphosphine (0.577 g, 2.2 mmol) was dissolved in dry tetrahydrofuran (20 mL) under argon and the solution cooled to 0–5° C. Diisopropyl azodicarboxylate (0.404 g, 2 mmol) was added dropwise and the mixture stirred at 0–5° C. for 20 min. before addition of 7-hydroxy-3,4-dihydro-1H-quinolin-2-one (0.326 g, 2 mmol) and 4-hydroxypiperidine-1-carboxylic acid tert-butyl ester (0.402 g, 2 mmol). The resulting mixture was stirred at ambient temperature for 18 h then evaporated to dryness under reduced pressure. Chromatography on SiO2, eluting with a gradient of ethyl acetate in 60–80° C. petroleum ether, gave the title compound (0.2 g, 29%) as a white solid.

1. temperaturethe solution cooled to 0–5° C
2. customthen evaporated to dryness under reduced pressure
3. washChromatography on SiO2, eluting with a gradient of ethyl acetate in 60–80° C. petroleum ether