Development of highly efficient asymmetric synthesis process using simple five-membered heterocycles

本研究的目的是建立一种利用双环“屋顶”的2-氨基醇、1，2-二胺和2-氨基硫醇及其衍生物进行不对称反应的方法，这些衍生物是由相应的三环2-恶唑烷酮、2-咪唑烷酮和2-噻唑烷酮衍生的，它们已被证明是以下金属催化的不对称反应的良好手性配体：1）“Roofed”2-亚胺硫醚-Pd（II）配合物催化的乙酸烯丙酯的不对称取代（烷基化、胺化）; 2）“Roofed“2-噻唑啉-Cu（II）配合物催化的不对称Diels-Alder反应; 3）“Roofed”cis-1，2-diamine-Ru（II）配合物催化的酮和亚胺的不对称转移氢化。

The aim of this research is to establish the methodology for excellent asymmetric reactions using bicyclic "roofed" 2-airino alcohols, 1,2-diamines and 2-aminothiols and their derivatives, derived from the corresponding tricyclic 2-oxazolidinones, 2-imidazolidinones and 2-thiazolidinones, and they have been proven to be good to excellent chiral ligands for following metal-catalyzed asymmetric reactions:1) "Roofed" 2-iminothioether-Pd (II) complex-catalyzed asymmetric substitution (alkylation, amination) of allylacetates.2) "Roofed"2-thiazoline-Cu (II) complex-catalyzed asymmetric Diels-Alder reaction.3) "Roofed" cis-1,2-diamine-Ru (II) complex-catalyzed asymmetric transfer hydrogenation of ketones and imines.