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Decagram-Scale Synthesis of OSUAB-0284 (1)

有机合成与工艺文献分享 2025-05-22 06:10
文章摘要
本文介绍了OSUAB-0284的十克级合成方法，该化合物是治疗葡萄球菌感染，特别是耐甲氧西林金黄色葡萄球菌(MRSA)的临床前候选药物。研究目的是优化合成路线，避免早期引入成本较高的氟萘啶12，并解决合成过程中的非选择性环化和Heck反应转化率低的问题。通过调整保护基策略和优化反应条件，如降低Pd(OAc)2的负载量和反应温度，成功提高了合成效率和选择性。最终，研究实现了OSUAB-0284的高效合成，为后续的临床研究奠定了基础。
Decagram-Scale Synthesis of OSUAB-0284 (1)
查看文献： Decagram-Scale Synthesis of the Novel Bacterial Topoisomerase Inhibitor OSUAB-0284
查看期刊： Organic Process Research & Development
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