Pivaloyl chloride → 6-(benzyloxy)-7-(5-(4-fluorobenzyl)thiazol-2-yl)-1-(2-oxo-2-(4-pivaloylpiperazin-1-yl)ethyl)imidazo[1,2-a]pyrimidin-5(1H)-one

Participants

Reaction Conditions

Reaction Steps

A mixture of the product of example 112 (200 mg, 0.36 mmol) and DIPEA (50.94 mg, 0.39 mmol) in CH2Cl2 (10 ml) was stirred at 0° C. Then pivaloyl chloride (47.48 mg, 0.39 mmol) was added dropwise. The mixture was stirred at room temperature for 2 hours, after which saturated sodium bicarbonate was added and then extracted with ethyl acetate. The extracts were combined, washed with brine, and then dried over sodium sulfate. The product was purified by column chromatography (CH2Cl2/MeOH=10/1) to give the desired product (207 mg, 90% yield).

Provenance & Evidence