Nanotec-CU Center of Excellence on Food and Agriculture, Department of Chemistry, Faculty of Science, Chulalongkorn University Bangkok 10330, Thailand.
J Org Chem. 2017 Dec 15;82(24):13256-13262. doi: 10.1021/acs.joc.7b02357. Epub 2017 Nov 28.
The direct amination reaction of heterocyclic thiols has been developed in the presence of the nonhazardous photocatalyst Rose Bengal under irradiation of visible light. The reaction provides a straightforward approach to pharmaceutically and synthetically useful 2-aminobenzoxazole and 4-aminoquinazoline derivatives from the corresponding heterocyclic thiols with amines in good to excellent yields. Our photochemical reaction can be successfully adapted into a continuous flow reactor which is applicable for large-scale chemical industry. The key benefits of this reaction include the use of metal-free, low-cost Rose Bengal catalyst and practical operation (ambient temperature, open flask, and undried solvents).
在无害光催化剂 Rose Bengal 的照射下，开发了杂环硫醇的直接胺化反应。该反应提供了一种直接的方法，可从相应的杂环硫醇和胺中获得具有良好至优异收率的药物和合成有用的 2-氨基苯并恶唑和 4-氨基喹唑啉衍生物。我们的光化学反应可以成功地适应到连续流反应器中，适用于大规模的化学工业。该反应的关键优点包括使用无金属、低成本的 Rose Bengal 催化剂和实用操作（环境温度、开瓶和未干燥的溶剂）。
