Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences , Chongqing University , Chongqing 401331 , P. R. China.
Org Lett. 2018 Aug 17;20(16):4959-4963. doi: 10.1021/acs.orglett.8b02087. Epub 2018 Aug 7.
A simultaneous asymmetric Mannich reaction and the construction of axially chiral sulfone-containing styrenes in one pot from α-amido sulfones based on the waste-reuse strategy was demonstrated. A series of chiral β-amino diesters and axially chiral sulfone-containing styrenes with various functional groups were synthesized in good to excellent yields and enantioselectivities under mild conditions. In addition, this protocol has been successfully applied to synthesize the anti-HIV drug Maraviroc and chiral trichloro derivatives.
基于废物再利用策略，展示了一种从 α-酰胺砜出发，一锅法同时进行不对称 Mannich 反应和手性含砜苯乙烯的轴不对称构建。在温和条件下，以良好到优异的产率和对映选择性合成了一系列具有各种官能团的手性 β-氨基二酯和手性含砜苯乙烯。此外，该方案已成功应用于合成抗 HIV 药物马拉维若和手性三氯衍生物。
