4-Aminobenzoic Acid → 4-(4-(1-(2-cyano-1-cyclopropylethyl)-1H-pyrazol-4-yl)pyrimidin-2-ylamino)benzoic Acid

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Reaction Steps

A mixture of 3-(4-(2-chloropyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopropylpropanenitrile (2.74 g, 0.0100 mol), p-aminobenzoic acid (2.06 g, 0.0150 mol), and p-toluenesulfonic acid (1.5 g, 0.0085 mol) in dry 1,4-dioxane (80 mL) was refluxed overnight. The mixture was cooled to room temperature, filtered. The solid was washed with dioxane, air dried to yield the desired product as a racemic mixture (3.02 g, 80.58%). LCMS (M+H) 375.3.

Provenance & Evidence