A novel, short, and efficient synthetic pathway to 3-{4-[2-(3-chlorophenylamino)-pyrimidin-4-yl]-pyridin-2-ylamino}-propanol (CGP 60474) and a series of analogues was developed. The syntheticsequence consisted of a Negishi-type cross-coupling reaction in the key step followed by twosubsequent nucleophilic substitution reactions. This strategy represents a versatile and robustprotocol to access diverse analogues of the title compound for subsequent SAR studies as potentialphenylamino-pyrimidine type protein kinase C inhibitors.