反应详情

温度

100 °C

An oven-dried, nitrogen cooled 2 ml microwave vial was charged with ethyl 3-(6-chloro-1-trityl-1H-pyrazolo[4,3-c]pyridin-3-yl)propanoate (59 mg, 0.119 mmol), BrettPhos precatalyst (5 mg, 6.26 μmol), cesium carbonate (122 mg, 0.374 mmol) and 1-benzylurea (32 mg, 0.213 mmol), sealed under a nitrogen atmosphere, charged with Dioxane (0.5 ml) and heated to 100° C. for 16 hr. Filtered through celite, eluted with EtOAc, concentrated in vacuo and purified via flash chromatography (0-20% MeOH/DCM) to provide ethyl 3-(6-(3-benzylureido)-1-trityl-1H-pyrazolo[4,3-c]pyridin-3-yl)propanoate (38.7 mg, 0.063 mmol, 53.4% yield) as a yellow solid. MS ESI calc'd for C38H35N5O3 [M+H]+=610, found 610.

1. temperatureAn oven-dried, nitrogen cooled 2 ml microwave vial
2. customsealed under a nitrogen atmosphere
3. filtrationFiltered through celite
4. washeluted with EtOAc
5. concentrationconcentrated in vacuo
6. custompurified via flash chromatography (0-20% MeOH/DCM)