Zeng Bi-Shun, Yu Xinyi, Siu Paul W, Scheidt Karl A
Department of Chemistry, Center for Molecular Innovation and Drug Discovery, Chemistry of Life Processes Institute, Northwestern University, 2145 Sheridan Road, Evanston, IL 60208, USA.
Chem Sci. 2014 Jun;5(6):2277-2281. doi: 10.1039/C4SC00423J.
An enantioselective Pd-catalyzed 6--trig reaction for the synthesis of 2-aryl-chromenes has been developed. A systematic optimization of a TADDOL-derived ligand set resulted in the identification of a novel monodentate phosphoramidite-palladium catalyst that accesses 2-aryl--chromenes with high yield and enantioselectivity under mild conditions. The products obtained from this method can be transformed into biologically active compounds through functionalization of the chromene alkene.
已开发出一种用于合成2-芳基色烯的对映选择性钯催化6-三氟甲基化反应。对源自TADDOL的配体组进行系统优化，从而确定了一种新型单齿亚磷酰胺钯催化剂，该催化剂能在温和条件下以高收率和对映选择性得到2-芳基色烯。通过色烯烯烃的官能化，由该方法得到的产物可转化为生物活性化合物。
