Jiangsu Laboratory of Advanced Functional Material, School of Chemistry and Materials Engineering, Changshu Institute of Technology, Changshu 215500, China.
Molecules. 2017 Sep 11;22(9):1531. doi: 10.3390/molecules22091531.
Efficient, eco-friendly and sustainable access to 3,4-dihydropyrimidin-2(1)-ones directly from alcohols under microwave and solvent-free conditions has been reported. The practical protocol involves heteropolyanion-based catalyzed oxidation of alcohols to aldehydes with NaNO₃ as the oxidant followed by cyclocondensation with dicarbonyl compounds and urea or thiourea in a two-step, one-pot manner. Compatibility with different functional groups, good to excellent yields and reusable catalysts are the main highlights. The utilization of alcohols instead of aldehydes is a valid and green alternative to the classical Biginelli reaction.
已经报道了一种在微波无溶剂条件下，从醇类物质直接高效、环保且可持续地合成 3,4-二氢嘧啶-2(1H)-酮的方法。该实用方案涉及基于杂多阴离子的催化氧化醇类物质为醛，以 NaNO₃作为氧化剂，然后与二羰基化合物和脲或硫脲在两步一锅法中环化缩合。该方法与不同官能团的兼容性、良好至优异的产率和可重复使用的催化剂是其主要特点。使用醇类物质代替醛类物质是对经典的比格列尼反应的一种有效且绿色的替代方法。
