反应详情

温度

0 °C

(R)-3-(5-(Benzyloxy)pyridin-2-yl)-2-(tert-butoxycarbonylamino)propanoic acid (0.19 g, 0.5 mmol), 4-(4-hydroxyphenyl)-N-(tetrahydro-2H-pyran-2-yloxy)-butanamide (0.14 g, 0.5 mmol), and DMAP (0.06 g, 0.5 mmol) were added into DCM (10 mL) and stirred at 0° C. for 10 min. A solution of DCC (0.12 g, 0.6 mmol) in DCM (5 mL) was added to the above-mentioned solution dropwise. The mixture was stirred from 0° C. at room temperature for 1 h (monitored by TLC). The white solid was removed and the filtrated was then evaporated in vacuo. Ethyl acetoacetate was added and the solid was again removed. The solution was evaporated in vacuo. The residue was purified by chromatography (EA:Hex=1:5) to give the title compound.

1. stirringThe mixture was stirred from 0° C. at room temperature for 1 h (monitored by TLC)
2. customThe white solid was removed
3. customthe filtrated was then evaporated in vacuo
4. additionEthyl acetoacetate was added
5. customthe solid was again removed
6. customThe solution was evaporated in vacuo
7. customThe residue was purified by chromatography (EA:Hex=1:5)