【摘 要】
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Trifluoromethyl-substituted dihydroquinazolinones are important structural motifs found in many pharmaceuticals and bioactive compounds.Notably, among these com
【机 构】
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DepartmentofChemistry,TianjinUniversityTianjin300072
【出 处】
：
中国化学会全国第十一届有机合成化学学术研讨会
论文部分内容阅读
Trifluoromethyl-substituted dihydroquinazolinones are important structural motifs found in many pharmaceuticals and bioactive compounds.Notably, among these compounds, DPC-961, DPC-963, DPC-082, and DPC-083 are nonnucleoside reverse transcriptase inhibitors (NNRTIs) that show promise for the treatment of HIV as well as new mutant strains of the virus.1 As a result of their important usefulness, developing new, highly enantiosetective methods for the construction of these compounds and analogues has become the subject of intensive research in the fields of synthetic and medicinal chemistry.Inspiration from these anti-HIV drugs, my research group developed a new enantioselective enynylation reaction by using trifluoromethyl-substituted dihydroquinazolinones as electrophilic substrates.Further synthetic transformation gave rise to the analogues of the anti-HIV drugs DPC-961 and DPC-083 (Figure 1).2 It is likely that the compounds prepared here will provide novel therapeutic agents and useful biological tools.
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