STEREOSELECTIVE SYNTHESIS OF POLYFUNCTIONAL AMINES

这项提案详细说明了为制定新战略而进行的研究 多官能团胺的立体选择性合成及其应用 含胺天然产物的全合成战略。这个 策略包括使用亲水性引发的环官能化 不饱和胺衍生物在体内的相对不对称诱导 环状体系和非环状体系的合成。靶分子 选定的具有重要的药理和生物学意义，以及 待开发的方法将有可能应用于 许多类型的其他重要的药理结构。举例 待调查的天然产品类型包括多取代哌啶 和全氢哒嗪生物碱和氨基酸，新的多官能团 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.