Novel diversely substituted 1-heteroaryl-2-imidazolines for fragment-based drug discovery

作者：Krasavin Mikhail^*

来源：Tetrahedron Letters, 2012, 53(23): 2876-2880.

DOI：10.1016/j.tetlet.2012.03.122

• Fragment-based drug discovery
• 2-Imidazolines
• Rule of Three
• Buchwald-Hartwig reaction
• 2-Haloazines
• Imidazoline dimers

A palladium-catalyzed Buchwald-Hartwig arylation protocol has been applied to achieve high-yielding N-heteroarylation of a diverse set of privileged 2-imidazolines. The resulting compounds are of interest as a novel type of molecular tool for fragment-based drug discovery. The potential for combining two 2-imidazoline moieties in a heteroarene-linked dimer via sequential Pd-catalyzed arylation has been demonstrated.

• 出版日期2012-6-6