4-(Trifluoromethyl)phenylboronic acid → 2-(Ethyloxy)-2-oxoethyl 4-{5-[4-(trifluoromethyl)phenyl]-2-pyridyl}-1-piperazinecarboxylate

Participants

Reaction Steps

The process is performed according to the procedure described in Example 1 (step 1.3.). Starting with 4 g (10.75 mmol) of 2-(ethyloxy)-2-oxoethyl 4-(5-bromo-2-pyridyl)-1-piperazinecarboxylate, obtained in step 3.3. of Example 3, 5.50 g (28.96 mmol) of 4-(trifluoromethyl)phenylboronic acid, 9.12 g (42.99 mmol) of hydrated potassium phosphate and 1.24 g (1.07 mmol) of tetrakis(triphenylphosphine)palladium, and after chromatography on silica gel, eluting with a 30/70 mixture of ethyl acetate and cyclohexane, 2.78 g of product are obtained in the form of a white solid.

Provenance & Evidence