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，化学和 有机金属立体选择性还原N-亚氨基衍生物 试剂。新型N-硅基-N-硅氧烷-，N-硼氧亚胺AS的合成 以及它们与非手性和手性有机硼烷试剂的还原反应 提出了获取伯胺的方法。N-酰基-AND的化学 N-水飞蓟胺及其相应的烯胺将更加深入 研究了一种制备氨基醇的替代路线 氢化硼化反应，这一方法只得到了有限的 请注意。计划继续研究Beta-烷基化 和N-取代亚氨基衍生物的硅烷化，这提供了 重要的β-取代胺和酮的可能性。这个 有计划的战略将用于综合重要的 药理化合物，如拟交感神经制剂，如阿尔法- 以及β-苯乙胺和苯基异丙胺。

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.