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将三维结构引入药物分子已被证明显著提升临床成功率。药物分子的晚期饱和化为该转化提供了直接途径。然而,实现芳香环的选择性且可控还原仍具挑战性,尤其是在存在多个芳香环的情况下。本文报道了苯环和吡啶环的可切换且化学选择性氢化。该方案结合片段筛选技术,在多样化底物中进行了综合研究。该方法便捷获得多种环己烷和哌啶化合物,这些结构广泛存在于多种生物活性分子和药物中。此外,该方法为药物晚期可切换饱和化开辟了有前景的应用途径,有助于提高sp的比例
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Fuhao Zhang
Himadri Sekhar Sasmal
Debanjan Rana
Journal of the American Chemical Society
University of Münster
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Zhang 等人(周四,)研究了该问题。
www.synapsesocial.com/papers/68e62eabb6db6435875c154f — DOI: https://doi.org/10.1021/jacs.4c05883
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