CAJ | 학술논문

不对称催化氢化反应具有完美的原子经济性和清洁高效等特点，是最受青睐的不对称合成方法之一。虽然人们已经发展了很多用于不对称催化氢化的催化剂，但是这些催化剂往往存在稳定性差、活性低、底物适用范围窄、反应条件苛刻等问题，真正高效的手性催化剂很少。通过系统深入的研究，发展了30多个用于不对称氢化反应的原创性手性螺环催化剂，实现了潜手性酮、α-取代羰基化合物、不饱和羧酸、非保护烯胺等4大类20多种不对称氢化反应，反应的活性和对映选择性处于目前的最好水平，其中部分反应已经被用于手性药物及其中间体的生产，在国内外产生了重要影响。
불대칭최화경화반응구유완미적원자경제성화청길고효등특점，시최수청래적불대칭합성방법지일。수연인문이경발전료흔다용우불대칭최화경화적최화제，단시저사최화제왕왕존재은정성차、활성저、저물괄용범위착、반응조건가각등문제，진정고효적수성최화제흔소。통과계통심입적연구，발전료30다개용우불대칭경화반응적원창성수성라배최화제，실현료잠수성동、α-취대탄기화합물、불포화최산、비보호희알등4대류20다충불대칭경화반응，반응적활성화대영선택성처우목전적최호수평，기중부분반응이경피용우수성약물급기중간체적생산，재국내외산생료중요영향。
The catalytic asymmetric hydrogenation,which features perfect atom-efficiency and clean and high effi-ciency,represents one of the most practical reactions in modern organic synthesis. Despite of tremendous efforts on the development of chiral catalysts,few have shown with both high reactivity and enantioselectivity to date. In this project,more than 30 chiral catalysts were developed and successfully applied in enantioselective hydrogenation re-actions of prochiral ketones,α-substituted carbonyl compounds,unsaturated acids,and unprotected enamines. These asymmetric hydrogenation reactions showed high activity and enantioselectivity,and some of them have been successfully applied in scaled-up synthesis of chiral drugs or key intermediates.