Japan JSPS Program: Enantioselective Total Synthesis of (+)- Catharanthine

该奖项支持日本东京大学Eric Zylstra博士获得为期24个月的日本科学促进会（JSPS）博士后奖学金。Zylstra博士将与东京大学药学院教授Tohru Fukuyama博士合作进行一个名为“长春花碱的对映选择性全合成”的研究项目。该研究将为开发抗肿瘤药物长春花碱提供一条直接、有效的途径。虽然这种化合物在化疗中有很长的使用历史，但其结构的复杂性阻碍了类似物的制备。长春花碱的一种常用合成策略是将长春花碱或类似长春花碱的前体与结构相关化合物长春花碱偶联。研究将进行一些新的钯方法学组装长春碱骨架的有效性。这将导致更直接、更有效的合成途径的发展，使其和结构相似的类似物更容易用于制备新的、更有效的长春花碱类似物。＊＊＊

Zylstra 9803688 This award supports a 24 month Japan Society for the Promotion of Science (JSPS) Postdoctoral Fellowship for Dr. Eric Zylstra at the University of Tokyo in Japan. Dr. Zylstra will work with Dr. Tohru Fukuyama, Professor, Faculty of Pharmaceutical Sciences, University of Tokyo on a research project entitled "Enantioselective Total Synthesis of Vinblastine." The proposed research will provide a direct, efficient route to the antitumor drug vinblastine. Although this compound has a long history of use in chemotherapy, its structural complexity hinders the preparation of analogs. One commonly chosen synthetic strategy toward vinblastine is the coupling of catharanthine or a catharanthine-like precursor with the structurally-related compound vindoline. Investigations will be undertaken on the usefulness of some novel palladium methodology for assembling the vinblastine skeleton. This should lead to development of a more direct, efficient route to its synthesis making it, and structurally similar analogs, more readily available for the preparation of new, more potent vinblastine analogs. ***