The synthesis of new 3'-deoxy-3'-[4-(pyrimidin-1-yl)methyl-1,2,3-triazol-1-yl]-thymidine 6a-f, from 3'-azido-3'-deoxy-5'-O-monomethoxytrityl-thymidine is described. The key step is the 1,3-dipolar cycloaddition between the azido group of the protected AZT 3 and N-1-propargylpyrimidine derivatives 2a-f. All new derivatives 6a-f were evaluated for their inhibitory effects against the replication of HIV-1 (IIIB), HIV-2 (ROD). No marked activity was found.

Synthesis of 3'-Deoxy-3'-[4-(pyrimidin-1-yl)methyl-1,2,3-triazol-1-yl]thymidinevia 1,3-Dipolar Cycloaddition. -6 Thymidine derivatives of type (IV) are prepared and tested for their inhibitory effects against the replication of HIV-1 (IIIB) and HIV-2 (ROD). No marked activity is found. -(TOURIRTE, M.; OULIH, T.; LAZREK*, H. B.; BARASCUT, J. L.; IMBACH, J. L.; ALMASOUDI, N. A.; Nucleosides,