Scale-Up of the Synthesis of a Pyrimidine Derivative Directly on Solid Support

Abstract

The solid-phase synthesis of 4-(2-amino-6-phenylpyrimidin-4-yl)benzamide, a compound obtained through combinatorial chemistry and parallel synthesis, can be scaled up directly on solid support in excellent yields and high purity. By applying highly loaded aminomethyl polystyrene as solid support, a good ratio between the product and the starting resin is achieved. For comparison, the synthesis was also performed in solution. The solid-phase synthesis approach has the advantage that the desired compound is easily and quickly accessible in sufficient quantities for early development demands.