Design And Synthesis Of Triazole HIV-1Non-nucleoside Reverse Transcriptase Inhibitors

HIV-l non-nuclear nucleoside reverse transcriptase inhibitors is a kind of very importanttherapeutic agents in the treatment of AIDS, new type, high efficiency, low toxicity, broad-spectrum resistance to drug resistance of research and development of nuclear nucleosidereverse transcriptase inhibitors is currently one of the important direction of anti-hiv drugsresearch.This paper used the "butterfly" structure and TMC VRX-480773-480773as the leadcompounds, the existing non-nuclear nucleoside reverse transcriptase inhibitors based onstructure analysis,4-trichlorobenzene pyrimidine ring or one to three nitrogen substituted1,2,3-triazole ring, and by modifying the structure, design a variety of structural types ofnovel1,2,3-triazole reverse transcriptase inhibitors. In this paper, the synthetic route oftarget compounds containing sulfur, especially for carbon carbon several synthetic route ofthree key target compounds were explored. In the synthesis of the compounds such assulfur ether, amide tried a variety of synthetic methods, the reaction conditions wereoptimized. The series ii compound were designed a simple reaction conditions, the series iiiwere not successful builded, but the wor of series iii can be a good reference for the later.Finally11target compound and32kinds of new compounds were synthesized by multi-step, and through the nuclear magnetic resonance (NMR) and mass spectrometry to thestructure identification.