Synthetic Development of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) as Anti-HIV Drugs: Efavirenz and its Derivatives

Background: The acquired immune deficiency syndrome (AIDS) has long been a globally fetal disease which brings much pain to patients. To minimize the suffering of its victims, corresponding drug therapy has been developed for several generations. Objective: One efficient kind of drugs, non-nucleoside reverse transcriptase inhibitors (NNRTIs), is briefly reviewed. The most representative molecule efavirenz which is still employed as first-line anti-HIV drug in many countries is investigated about its enantioselective synthesis; its derivatives (DPC 083, DPC 961) are widely studied with more details. Conclusion: From the development of this asymmetric catalysis, it can be concluded that new catalysis systems with higher efficiency, lower catalyst loading, and lower cost are pursued and discovered. Several kinds of synthesis strategies are summarized and much emphasis is placed on the construction of trifluoromethylcontaining tertiary carbon chiral center.