4-Aminobenzoic Acid → 4-(4-(1-(2-cyano-1-cyclopentylethyl)-1H-pyrazol-4-yl)-5-methoxypyrimidin-2-ylamino)benzoic Acid

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Reaction Steps

A mixture of 3-(4-(2-chloro-5-methoxypyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile (120 mg, 0.36 mmol), p-aminobenzoic acid (74.4 mg, 0.542 mmol), and p-toluenesulfonic acid (53 mg, 0.31 mmol) in dry 1,4-dioxane (3 mL) was refluxed overnight. The mixture was cooled to room temperature. The resulting solid was filtered and washed with dioxane to give the desired product as a racemic mixture (120 mg, 76.7%). LCMS (M+H) 433.3.

Provenance & Evidence