Four-Component Reactions for a New Diastereoselective Synthesis of Chiral Quaternary Centers

The one-pot preparation of chiral homoallylic alcohol and amine derivatives was easily achieved by carbocupration of alkynyl sulfoxides followed by an in situ zinc homologation and reaction with aldehydes or imines. In this process, three new carbon−carbon bonds were created as well as quaternary and tertiary chiral centers with excellent diastereo- and enantioselectivities.

通过对炔基亚砜进行碳铜化反应，随后开展原位锌同系化并与醛或亚胺发生反应，可便捷实现手性高烯丙基醇与胺衍生物的一锅法制备。在该反应体系中，可生成三个全新的碳-碳键，同时构建出兼具优异非对映选择性与对映选择性的季手性中心及叔手性中心。