Iridium-catalyzed intramolecular CN and CO/S cross-coupling reactions: Preparation of benzoazole derivatives |
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| Institution: | 1. Department of Neurology, Graduate School of Medical Sciences, Kumamoto University, Kumamoto, Japan;2. Department of Medicine (Neurology and Rheumatology), Shinshu University School of Medicine, Matsumoto, Japan;3. Department of Morphological and Physiological Sciences, Graduate School of Health Sciences, Kumamoto University, Kumamoto, Japan;4. Pfizer Japan Inc., Tokyo, Japan |
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| Abstract: | The irdium-catalyzed intramolecular arylcarbon-hetero cross-coupling reactions with o-haloarylamides or o-haloarylamidine have been effectively achieved using KOAc and just 1 mol% catalyst. The Ir(cod)Cl]2 was proved to be more potential for smoothly assembling functional structures benzimidazoles, benzoxazoles and benzothiazoles, which was superior to Cu- and Pd-catalyzed systems. Simultaneously, a concise and efficient synthesis of tafamidis was developed in 5-g scale. |
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| Keywords: | Iridium Catalysis Intramolecular cross-coupling Benzoazole |
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