CuSCN催化格氏试剂与四氯锰酸二锂取代查尔酮的共轭加成反应及其生物活性研究

Mohan B. Kale, S. B. Jagtap, S. Devkate
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引用次数: 0

摘要

报道了硫氰酸铜催化格氏试剂与取代查尔酮的区域选择性1,4加成反应。采用四氯锰酸二锂均相溶液,用锰催化镁的金属化。在氮气气氛和较低温度下,对取代的查尔酮衍生物进行区域选择性加成,生成产率较高的1,4加成产物。用硫氰酸铜作催化剂,观察到四氯锰酸二锂中的锰取代格氏试剂中的镁,以1,4加成方式选择性地加入。研究了在无二硫四氯锰酸盐试剂的情况下的反应过程,得到了1,2加成和1,4加成的混合产物。在四氯锰酸二酯试剂存在下,得到了良好的区域选择性和较高的收率。所有化合物对金黄色葡萄球菌(革兰氏阳性)、大肠杆菌(革兰氏阴性)和黑曲霉的抑菌活性进行了评价。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Study of CuSCN Catalyzed Conjugate Addition Reactions of Grignard Reagents to Substituted Chalcones with Dilithium Tetrachloromanganate and their Biological Activities
The regioselective 1,4-addition reactions of copper thiocyanate catalyzed Grignard reagents to the substituted chalcones are reported. The homogeneous solution of dilithium tetrachloromanganate is used to transmetallate magnesium by using manganese. It adds regio-selectively to substituted chalcone derivatives and forms 1,4-addition products with higher yield under nitrogen atmosphere and at a lower temperature. It have been observed that manganese from dilithium tetrachloromanganate reagent replaces magnesium from Grignard reagent and adds regioselectively by 1,4-addition manner utilizing copper thiocyanate as a catalyst. The course of the reaction in the absence of dilithium tetrachloromanganate reagent was also studied and obtained a mixture of 1,2-addition and 1,4-addition products. In presence of dilithium tetrachloromanganate reagent, a good regio-selectivity and higher yield of desired 1,4-addition product were obtained. All the synthesized compounds were also evaluated for their antibacterial activity against Staphylococcus aureus (Gram-positive), Escherichia coli (Gramnegative) and antifungal activity against Aspergillus niger.
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