基于异斯特维醇的新型伯胺-方酰胺催化的高对映选择性Michael加成反应

Highly Enantioselective Michael Addition Catalyzed by New Primary Amine-Squaramide Organocatalysts

新型双功能伯胺-方酰胺能有效催化醛与马来酰亚胺的不对称Michael加成反应.应用此法,可简便地制备一系列取代的琥珀酰亚胺衍生物,并能以高产率(高达98%)和优秀的对映选择性(高达>99%ee)分别得到相应加成产物的两个异构体.

The asymmetric Michael addition reaction of α,α-disubstituted aldehydes to maleimides catalyzed by new bifunctional primary amine-squaramides has been developed. This organocatalytic asymmetric reaction provides easy access to functionalized succinimides with a broad substrate scope. Both enantiomers of desired succinimide derivatives were obtained in good to excellent yields（up to 98%） with excellent enantioselectivities（up to99% ee）