Synthesis of Uracil Derivatives Using Halogen-Magnesium Exchange

Significance

Derivatives of nucleobases like uracil and purin often display a useful biological activity. In this protocol, no preliminary protection of uracil is required, thus the method is one of the operationally most simple ones for the preparation of 5- and 6-substituted uracils. The utility of this method in the synthesis of biologically active molecules is demonstrated by the preparation of antiviral compounds emivirine. The same protocol was successfully applied to the functionalization of 6-iodopurine.