STEREOCHEMICAL CONTROLLED SYNTHESIS OF BIOLOGICALLY ACTIVE AMINES

我们将继续开发新的和通用的合成方法 胺，特别是生物活性胺的化学和生物活性， N-亚氨基衍生物有机金属立体选择性还原 试剂 新型N-硅基-N-硅氧基-，N-硼氧基亚胺的合成 以及它们与非手性和手性有机硼烷试剂的还原， 得到伯胺，提出。 N-酰基-和 N-甲硅烷基亚胺及其相应的烯胺将更深入地 研究作为制备氨基醇的替代路线， 硼氢化反应，一种仅受到有限关注的方法， 关注 计划继续研究β-烷基化 和N-取代的亚氨基衍生物的甲硅烷基化，其提供 重要的β-取代胺和酮的可能性。 的 计划的战略将用于综合重要的 药理学化合物如拟交感神经药如α- 和β-苯乙基胺和苯基异丙基胺。

We sill continue to develop new and general methods for the synthesis of amines, in particular biological active amine, the chemo- and stereoselective reduction of N-iminoderivatives with organometallic reagents. The synthesis of new N-silyl- N-silyloxi-, N-boryloxyimine as well as their reduction with achiral and chiral organoborane reagents to obtain primary amines, is proposed. The chemistry of the N-acyl- and N-silylimines and their corresponding enamines will be more deeply studied as an alternative rout for the preparation of amino alcohols by the hydroboration reaction, an approach which has received only limited attention. It is planned to continue to investigate the Beta-alkylation and silylation of the N-substituted imino derivatives, which offer the possibility of important Beta-substituted amines and ketones. The planned strategies will be used for the synthesis of important pharmacological compounds such as sympathomimetic agents such as alpha- and Beta-phenylethyl amines and; phenylisopropylamines.