Innate pharmacophore assisted selective C-H functionalization to therapeutically important nicotinamides
Innate pharmacophore assisted selective C-H functionalization to therapeutically important nicotinamides
复制标题
固有药效团辅助选择性 C-H 功能化对治疗上重要的烟酰胺
DOI：
10.1039/c9qo00170k
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发表时间：
2019
影响因子：
5.4
通讯作者：
Shengkun Li
中科院分区：
文献类型：
--
作者：
Zehua Song;Guotong Wang;Wei Li;Shengkun Li
确定了预先验证的药效团2-(2-恶唑烷基)苯胺作为先天导向基团在烟酰胺的C-H醚化和胺化反应中的应用，以有效地合成药物和农用化学品类分子。首先使用复杂的铜盐变体完成了烟酰胺的操作简单和区域选择性的C-H官能化。所有使用的特定程序都很容易使用，不需要外部氧化剂或配体。强调了通过快速合成烟酸相关药物或类似物来替代合成地氟非尼康的可行性。
The application of the pre-validated pharmacophore 2-(2-oxazolinyl)aniline as an innate directing group in the C–H etherification and amination of nicotinamides for the efficient synthesis of drug- and agrochemical-like molecules was determined. An operationally simple, and regioselective C–H functionalization of nicotinamides was first accomplished using a complicated variation of copper salts. All the specific procedures used were easy to utilize, without external oxidants or ligands. The feasibility is highlighted using an alternative synthesis of diflufenican with a rapid synthesis of niacin related pharmaceuticals or analogues.