The winning team reached the terra incognita: Enantioselective synthesis of ferrocene 1,3-derivatives via distal C-H activation by Pd(II)/norbornene cooperative catalysis

Together they solved the cold case! Activation of the distal C-H bonds of ferrocene and its stereoselective functionalization is not a dream anymore. Here we report, regio-and stereo selective catalytic distal C-H functionalization of ferrocenes actualizing the synthesis of ferrocene-1,3-derivatives by a Catellani-type reaction. The winning Pd/norbornene catalyst combination is able to reach hitherto inaccessible reaction site of ferrocene and accomplishes the regio-and stereoselective arylation of ferrocenylmethylamine. The ligand controlled synergistic Pd/norbornene metal-organic cooperative catalysis under aerobic conditions successfully achieves the synthesis of 30 ferrocene-1,3 derivatives in moderate to good yields and with high enantioselectivity in the substrates scanned.