反应详情

The above prepared ((cis)-2,6-dimethyl-morpholin-4-yl)-(5-hydroxy-benzofuran-2-yl)-methanone (0.150 g, 0.545 mmol) was dissolved in 2.7 mL of THF and treated successively at 10° C. with 1-isopropyl-piperidin-4-ol (0.156 g, 2 eq.), triphenylphosphine (0.285 g, 2 eq.) and DIAD (0.212 mL, 2 eq.), and the mixture then kept at ambient temperature for another 3 h. Pouring onto crashed ice/NH4Cl, twofold extraction with AcOEt, washing with water, drying over sodium sulfate, and evaporation of the solvents, followed by two flash chromatographies (SiO2, NEt3/AcOEt=4/96 and CH2Cl2/MeOH=9/1), yielded eventually 0.140 g of the title compound as colorless oil.

1. additionPouring
2. extractionice/NH4Cl, twofold extraction with AcOEt
3. washwashing with water
4. dry with materialdrying over sodium sulfate, and evaporation of the solvents