Room temperature Palladium-Catalyzed C─H Functionalization of Benzothiazole with Iodo(Hetero)Arenes

A versatile synthetic protocol involving the room temperature direct arylation of benzothiazole with a wide variety of iodo(hetero)arenes under palladium-catalyzed conditions and promoted by HFIP as the reaction solvent has been presented herewith. An in-situ one-pot sequential HFIP promoted selective iodination of (hetero)arenes followed by Pd-catalyzed direct arylation of benzothiazole has also been disclosed. Synthesis of PMX 610 (antitumor agent) analog has been disclosed and also CJM 126 (antitumor agent) has been synthesized.