科研之友
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摘要
An organocatalytic enantioselective Michael addition/aza-cydization cascade reaction of aldehydes with 2-amino-beta-nitrostyrenes has been developed for the construction of fully substituted chiral tetrahydroquinolines. The reaction, promoted by diphenylprolinol TMS ether as an organocatalyst, generated the chiral tetrahydroquinolines in good to high yield with excellent diastereo- and enantioselectivities (up to >30:1 dr, >99% ee). The method also provided an alternative access to chiral 1,4-dihydroquinolines, which are difficult to synthesize by other methodologies.
- 出版日期2014-9-5
