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Concise Synthesis of a Potential 5-Lipoxygenase Activating Protein (FLAP) Inhibitor and Its Analogs through Late-Stage Alkene Dicarbofunctionalization

机译:简化合成潜在的5-脂氧基酶活化蛋白(瓣)抑制剂及其通过后阶烯烃二官能化的类似物

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摘要

We report a five-step synthesis of the biologically important 1,1-diarylalkane 1, a potential 5-lipoxygenase activating protein (FLAP) inhibitor that was synthesized previously in 12 steps. In this synthesis, we apply a three-component alkene dicarbofunctionalization reaction as a key final step to assemble the potential FLAP inhibitor 1 from commercially available starting materials. In addition, we also report the synthesis of a variety of new analogs of the inhibitor 1 and its regioisomer.
机译:我们报告了生物学上重要的1,1-二芳基链烷1的五步合成,潜在的5-脂氧基酶活性蛋白(瓣膜)抑制剂,其先前在12步中合成。 在该合成中,我们将三分组分烯烃二官能化反应应用是从市售原料组装潜在的皮瓣抑制剂1的关键最终步骤。 此外,我们还报告了抑制剂1的各种新类似物的合成及其可抑制剂。

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