Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431004, MS, India.
Bioorg Med Chem Lett. 2013 May 1;23(9):2632-5. doi: 10.1016/j.bmcl.2013.02.099. Epub 2013 Mar 4.
It is the first report of 1,3,4,5-tetrasubstituted 1,2,3,6-tetrahydropyrimidines derivatives, catalyzed by ZrOCl2. The mild reaction conditions, excellent yields in shorter reaction time and evasion of cumbersome workup procedures make this process economically lucrative for industrial application. The novelty and highlight of the present method is the promising antibacterial and antifungal activity shown by compounds (4a, 4b, 4e, 4f, 4h and 4l) compared to standard.
这是首例由 ZrOCl2 催化的 1,3,4,5-四取代 1,2,3,6-四氢嘧啶衍生物的报道。温和的反应条件、较短反应时间内的优异产率以及避免繁琐的后处理步骤,使该工艺在工业应用方面具有经济优势。与标准品相比,本方法的新颖性和亮点在于化合物(4a、4b、4e、4f、4h 和 4l)表现出的有前景的抗菌和抗真菌活性。