We have discovered a 3-bromo-7-phenoxypyrazolo[1,5-a]pyrimidine intermediate that allows for the direct sequential funtionalization of the 3-position and 7-position of a pyrazolo[1,5-a]pyrimidine scaffold. The intermediate and general method described herein offer an improvement over prior methods, particularly in cases where multiple unique 3-aryl substituents are to be incorporated in conjunction with multiple unique 7-amino substituents.
Bibliographical noteFunding Information:
The authors wish to acknowledge the members of the Antiviral Discovery Performance Unit, as well as the Analytical and Separations groups at GlaxoSmithKline for their support and camaraderie. This work was financially supported by GlaxoSmithKline.
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