STEREOSELECTIVE SYNTHESIS OF POLYFUNCTIONAL AMINES

该提案详细介绍了为制定新战略而进行的研究， 多官能胺立体选择性合成及其应用 含胺天然产物的全合成策略。 的 该策略涉及使用亲电试剂引发的环官能化 的不饱和胺衍生物的相对不对称诱导， 环状和非环状体系的合成。 靶分子 所选药物具有显著的药理学和生物学重要性， 拟开发的方法有可能应用于 许多其他类型的重要结构。 的实例 待研究的天然产物类型包括多取代的哌啶 和全氢哒嗪生物碱和氨基酸， 用于抗生素和有毒蘑菇的氨基酸，以及氨基糖 抗肿瘤抗生素的成分。

This proposal details research for development of a new strategy for stereoselective synthesis of polyfunctional amines and application of this strategy to the total synthesis of amine-containing natural products. The strategy involves the use of electrophile-initiated cyclofunctionalization of unsaturated amine derivatives to effect relative asymmetric induction in the synthesis of both cyclic and acyclic systems. The target molecules selected have significant pharmacological and biological importance, and the methods to be developed would have the potential for application to many types of other pharmacologically important structures. Examples of natural product types to be investigated include polysubstituted piperidine and perhydropyridazine alkaloids and amino acids, novel polyfunctional amino acids for antibiotics and toxic mushrooms, and amino sugar constituents of antitumor antibiotics.