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Total syntheses of bryostatins: Synthesis of two ring-expanded bryostatin analogues and the development of a new-generation strategy to access the C7-C27 fragment

机译:bryostatins的总合成:两种环膨胀的bryostatin类似物的合成以及开发新一代访问C7-C27片段的策略

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Herein, we report the synthesis of novel ring-expanded bryostatin analogues. By carefully modifying the substrate, a selective and high-yielding Ru-catalyzed tandem enyne coupling/Michael addition was employed to construct the northern fragment. Ring-closing metathesis was utilized to form the 31-membered ring macrocycle of the analogue. These ring-expanded bryostatin analogues possess anticancer activity against several cancer cell lines. Given the difficulty in forming the C16-C17 olefin at a late stage, we also describe our development of a new-generation strategy to access the C7-C27 fragment, containing both the ring B and C subunits.
机译:在这里,我们报告了新型环膨胀的bryostatin类似物的合成。通过仔细修饰底物,采用选择性和高产率的Ru催化的串联烯炔偶联/ Michael加成来构建Northern片段。利用闭环复分解形成类似物的31元环大环。这些环膨胀的抑菌素类似物具有针对几种癌细胞的抗癌活性。鉴于在后期阶段难以形成C16-C17烯烃,我们还描述了开发新一代策略以开发同时包含环B和C亚基的C7-C27片段的方法。

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