Water → HCID 86721281, compound

Participants

Reaction Steps

To a solution of triethyl phosphonoacetate (0.026 ml, 0.13 mmol) in THF (2.0 mL) was added sodium hydride (55 wt % paraffin oil, 5.15 mg, 0.13 mmol) at 0° C., and the mixture was stirred at room temperature for 15 min. To the reaction mixture was added a solution of the compound (40 mg, 0.12 mmol) obtained in step 3 in THF (2.0 mL) at 0° C., and the mixture was stirred at room temperature for 5 hr. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer was washed with water and dried, and the solvent was evaporated under reduced pressure, and the residue was crystallized from diethyl ether-hexane to give ethyl(E)-3-(2-(1-(tert-butyl)-5-(4-methoxyphenyl)-1H-pyrazol-4-yl)thiazol-4-yl)acrylate (12.2 mg, 0.030 mmol, 25.3%) as a white powder.

Provenance & Evidence