Department of Medicinal Chemistry, China Pharmaceutical University , Nanjing 210009, China.
Org Lett. 2014 Jan 3;16(1):42-5. doi: 10.1021/ol402965d. Epub 2013 Dec 12.
An intermolecular C-H amination of 1-aryl-1H-pyrazol-5(4H)-ones was achieved under mild reaction conditions, using a low catalyst loading and with a broad scope of aminating reagents. This protocol not only provides the first example of rhodium(III)-catalyzed intermolecular aromatic C-H amination directed by an intrinsic functionality of the substrate/product but also features aminating an existing drug with either primary or secondary N-benzoate alkylamines as the coupling partners.
在温和的反应条件下，通过使用低催化剂负载量和广泛的胺化试剂，实现了 1-芳基-1H-吡唑-5(4H)-酮的分子间 C-H 胺化反应。该方案不仅提供了首例铑(III)催化的分子间芳基 C-H 胺化反应，其导向基团为底物/产物的固有官能团，而且还具有用现有药物作为偶联试剂，以伯或仲 N-苯甲酸盐烷基胺进行胺化的特点。
