Del Fiandra Claudia, Moccia Maria, Adamo Mauro F A
Centre for Synthesis and Chemical Biology (CSCB), Department of Pharmaceutical and Medicinal Chemistry, Royal College of Surgeons in Ireland, 123 St Stephen's Green, Dublin 2, Ireland.
Org Biomol Chem. 2016 Mar 21;14(11):3105-11. doi: 10.1039/c6ob00154h. Epub 2016 Feb 24.
Cyclopropane esters holding two quaternary centres were prepared in high yields, complete diastereoselection and up to 83% ee. The reaction described herein entailed reacting (Z)-3-substituted-2-(4-pyridyl)-acrylonitrile, a reactive class of Michael acceptor, with 2-bromomalonate esters in the presence of Cinchona derived phase-transfer catalysts. The reaction allowed multi-gram preparation of the desired products.
含有两个季碳中心的环丙烷酯以高产率、完全的非对映选择性和高达83%的对映体过量率被制备出来。本文所述的反应涉及使(Z)-3-取代-2-(4-吡啶基)丙烯腈（一种活性类别的迈克尔受体）与2-溴丙二酸酯在金鸡纳衍生的相转移催化剂存在下反应。该反应能够以多克规模制备所需产物。
