Direct Heteroarylation of Tautomerizable Heterocycles into Unsymmetrical and Symmetrical Biheterocycles via Pd/Cu-Catalyzed Phosphonium Coupling

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• 作者：Abhishek Sharma ; Dipak Vachhani ; Erik Van der Eycken
• 刊名：Organic Letters
• 出版年：2012
• 出版时间：April 6, 2012
• 年：2012
• 卷：14
• 期：7
• 页码：1854-1857
• 全文大小：273K
• 年卷期：v.14,no.7(April 6, 2012)
• ISSN：1523-7052

文摘

The direct cross-coupling of tautomerizable heterocycles with various unfunctionalized heteroarenes has been achieved through PyBroP-mediated and Pd/Cu-catalyzed sequential C鈥揙H/C鈥揌 activation. The methodology allows a facile entry into novel diazine-azole biheterocyclic frameworks. Moreover, an unprecedented Pd-catalyzed phosphonium homocoupling of tautomerizable heterocycles was also developed to afford a direct synthetic route to symmetrical 1,2-, 1,3-, and 1,4-bidiazine units.