Synthesis of Heterocyclic Triads by Pd-Catalyzed Cross-Couplings and Evaluation of Their Cell-Specific Toxicity Profile

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• 作者：Joseph Salamoun ; Shelby Anderson ; James C. Burnett ; Rick Gussio ; Peter Wipf
• 刊名：Organic Letters
• 出版年：2014
• 出版时间：April 4, 2014
• 年：2014
• 卷：16
• 期：7
• 页码：2034-2037
• 全文大小：289K
• 年卷期：v.16,no.7(April 4, 2014)
• ISSN：1523-7052

文摘

Two complementary approaches for the preparation of linked 5-membered heterocycles were developed. The Pd-catalyzed Suzuki鈥揗iyaura cross-coupling with halogenated furan, thiophene, and selenophene led to higher overall yields, but C,H-bond activation was a more efficient strategy for the coupling at C(2) of oxazoles. Potency and selectivity of the final hydroxymethyl products in renal (A498), lung (NCI-H226), kidney (CAKI-1), and breast (MDA-MB-468, MCF7) carcinoma cell lines were determined.