Kevin Klaus Stefanoni, René Wilhelm
High Resolution Image Download MS PowerPoint Slide An unprecedented photocatalyzed radical C(sp 2 )–C(sp 3 ) alkylation protocol to prepare a range of substituted 3-alkylated indolizine derivatives, mediated by 2-mercaptothiazolidinium salts as radical sources and a new dyad-like Ruthenium complex as a photoredox catalyst, under green light irradiation, resulted in yields of up to 99%. The mild, robust, and chemoselective procedure employs inexpensive, air-insensitive, and readily accessible reagents, enabling convenient synthesis of the substituted indolizines. Moreover, different N -heteroarenes, such as 1 H -indoles and 2 H -indazoles, were successfully alkylated under the optimized conditions. The resulting alkylated products are scaffolds with significance for drug design in medicinal chemistry.