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

本研究的目的是利用由相应的三环2-恶唑烷酮、2-咪唑烷酮和2-噻唑烷酮衍生的双环2-芳基醇、1，2-二胺和2-氨基硫醇及其衍生物建立优良的不对称反应方法学，并且它们已被证明对以下金属催化的不对称反应具有良好的手性配体：1)“屋顶”2-亚胺硫醚-钯(II)络合物催化的不对称取代(烷基化，2)“有顶”的2-噻唑啉-铜(II)络合物催化的不对称Diels-Alder反应。3)“有顶的”顺-1，2-二胺-Ru(II)络合物催化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.