A NEW PROCEDURE FOR THE PHOSPHORYLATION OF NUCLEOSIDES: APPLICATION TO THE DISCOVERY OF INHIBITORS OF HIV INTEGRASE

A new phosphorylating agent for nucleosides, 2-O-(4,4′-dimethoxytrityl) ethylsulfonylethan-2′-yl-phosphate (1), has been developed by us. In the many examples studied by us, phosphorylation yields were found to be very high (about 90%). The procedure appears to be remarkably general and can be utilized for the phosphorylation of many biomolecules. Successful application of this phosphorylation method has contributed to the discovery of inhibitors of HIV integrase in our laboratory.