反应详情

20 mg of 7-(Pyridin-2-yl)quinolin-5-ol, 30 mg of ((R)-4-((S)-1-hydroxyethyl)-1-((S)-1-(4-methoxyphenyl)ethyl)pyrrolidin-2-one and 50 mg of triphenylphosphin was dissolved in 2 mL of DCM. 45 mg of DBAD was added and the mixture stirred for 14 h at room temperature. The mixture was diluted with DCM and extracted with 1N NaOH and water. The organic phase was concentrated in vacuo and dissolved in 0.5 mL of TFA and heated 30 min at 90° C. in the microwave. The mixture was purified with HPLC (XbridgeC18, MeOH/water, TFA) to yield after lyophilisation 21 mg of Example 6 as solid.

1. extractionextracted with 1N NaOH and water
2. concentrationThe organic phase was concentrated in vacuo
3. dissolutiondissolved in 0.5 mL of TFA
4. temperatureheated 30 min at 90° C. in the microwave
5. customThe mixture was purified with HPLC (XbridgeC18, MeOH/water, TFA)