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.
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.
Two methods for the one-pot synthesis of 2,5-diarylimidazoles by palladium-catalyzed direct C–H arylation of 1-substituted imidazoles with aryl bromides have been devised. The first method, promoted by copper(I) iodide, is best suited for electron-poor aryl bromides, and also allows the 2,5-diarylation of thiazole and oxazole. The use of xylene instead of DMA is the key for the efficiency of the second method, which gives the best results with electron-rich aryl bromides.
Room temperature Palladium-Catalyzed C─H Functionalization of Benzothiazole with Iodo(Hetero)Arenes