4.7 Article

Ligand-Dependent Site-Selective Suzuki Cross-Coupling of 3,5-Dichloropyridazines

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JOURNAL OF ORGANIC CHEMISTRY
卷 78, 期 15, 页码 7758-7763

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AMER CHEMICAL SOC
DOI: 10.1021/jo401096u

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General methods for the highly site-selective Suzuki monocoupling of 3,5-dichloropyridazines have been discovered. By changing the ligand employed, the preferred coupling site can be switched from the 3-position to the 5-position, typically considered the less reactive C-X bond. These conditions are applicable to the coupling of a wide variety of aryl-, heteroaryl-, and vinylboronic acids with high selectivities, thus enabling the rapid construction of diverse arrays of diarylpyradazines in a modular fashion.

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