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

Reverse transcriptase inhibitors plays a vital role in the trentment of AIDS recently. Because of the issue that problems of HIV drug, for example, resistance, adverse drug reactions and long-term medication costs, the development of new and efficient non-nucleoside reverse transcriptase inhibitors has become an important direction of anti-HIV drugs.The first chapter introduces the recent research progress of non-nucleoside reverse transcriptase inhibitors. And based on the existing structure of the non-nucleoside reverse transcriptase inhibitors, we design novel HIV-1 non-nucleoside reverse transcriptase inhibitors.We design the synthesis routes successfully. Amide, synthesized by aromatic amine and ethyl cyanoacetate, reacted with p-methoxybenzyl azide to give the corresponding 5-amino-1, 2, 3-triazole compounds. N- alkylation reaction of 5-amino-1,2,3-triazole compounds and brominated hydrocarbon achieved, and the reaction conditions were optimized. Then p-methoxybenzy, the protecting group, was removed in acid conditions to give the title compounds and 20 new compounds were prepared in a overall yield of 22.5%-45.5%. The structure of the title compounds were identified by NMR.