Laboratory of Molecular Engineering, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, 190 Kaiyuan Boulevard, The Science Park of Guangzhou, Guangdong 510530, China.
Angew Chem Int Ed Engl. 2013 Jun 3;52(23):6015-8. doi: 10.1002/anie.201302442. Epub 2013 Apr 22.
A general approach toward the asymmetric total synthesis of various aspidosperma alkaloids includes the combination of a C-H bond activation with a Heck-type coupling, and the stereo-controlled formation of piperidine and pyrrolidine rings as key steps. The feasibility of this approach was demonstrated with the total synthesis of aspidophytine in 18 steps from 4,4-disubstituted cyclohexanedione and 2,3-dimethoxyaniline.
一种通用的方法，用于各种阿皮斯多玛烷生物碱的不对称全合成，包括 C-H 键活化与 Heck 型偶联的结合，以及作为关键步骤的哌啶和吡咯烷环的立体控制形成。该方法的可行性通过从 4,4-二取代环己二酮和 2,3-二甲氧基苯胺出发，经 18 步反应全合成阿皮斯多菲汀得到了证明。
