Ethyl bromopyruvate → ethyl 2-(1-tert-butyl-5-(4-fluorophenyl)-1H-pyrazol-4-yl)thiazole-4-carboxylate

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Reaction Steps

A solution of the compound (710 mg, 2.56 mmol) obtained in Example 1, step 4 and ethyl bromopyruvate (0.322 mL, 2.56 mmol) in ethanol (15 mL) was stirred at 80° C. for 16 hr. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (solvent gradient; 3→50% ethyl acetate/hexane) to give ethyl 2-(1-tert-butyl-5-(4-fluorophenyl)-1H-pyrazol-4-yl)thiazole-4-carboxylate (50 mg, 0.108 mmol, 64.6%) as a white powder.

Provenance & Evidence