Dutta Subhradeep, Bhatt Kamal, Cuffel Fabian, Seidel Daniel
Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, Florida 32611, United States.
Synthesis (Stuttg). 2023 Aug;55(15):2343-2352. doi: 10.1055/a-2022-1511. Epub 2023 Apr 13.
Secondary alicyclic amines are converted to their corresponding ring-fused imidazoles in a simple procedure consisting of oxidative imine formation followed by a van Leusen reaction. Amines with an existing α-substituent undergo regioselective ring-fusion at the α'-position. This method was utilized in a synthesis of fadrozole.
仲脂环胺可通过一个简单的过程转化为其相应的稠合咪唑环,该过程包括氧化亚胺的形成,随后进行范鲁森反应。具有现有α-取代基的胺在α'-位进行区域选择性环融合。该方法被用于法倔唑的合成。