m-Chloroperbenzoic acid → 4-[4-(4-Fluorophenyl)-2-methyl-5-(2-methanesulfonyl-pyrimidin-4-yl)-3-oxo-2,3-dihydro-pyrazol-1-yl]-piperidine-1 carboxylic acid tert-butyl ester

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Reaction Steps

To a solution of 4-[4-(4-fluorophenyl)-2-methyl-5-(2-methylsulfanyl-pyrimidin-4-yl)-3-oxo-2,3-dihydro-pyrazol-1-yl]-piperidine-1 carboxylic acid tert-butyl ester, 11, (5.9 g, 12 mmol) in CHCl3 (200 mL) at 0° C. is added meta-chloroperbenzoic acid (4 g, 23.37 mmol). After stirring for 5 minutes, saturated sodium bisulfite (20 mL) is added and the reaction mixture stirred for an additional 5 minutes. The aqueous phase is extracted three times with CH2Cl2, the combined organic phases washed with saturated sodium bicarbonate, dried (MgSO4), filtered and concentrated in vacuo. The crude material is used without further purification.

Provenance & Evidence