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Iodine catalyzed one-pot synthesis of highly substituted N-methyl pyrroles via [3+2] annulation and their in vitro evaluation as antibacterial agents

机译:碘通过[3 + 2]环化催化一锅合成高取代度的N-甲基吡咯及其作为抗菌剂的体外评价

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摘要

A new class of highly substituted pyrroles have been synthesized via a simple, fast, and efficient method using environmentally friendly iodine catalyzed [3 + 2] annulation. N-Methyl-N-[(E)-1-(methylsulfanyl)-2-nitro-1-ethenyl]amine (NMSM) 1 and beta-nitrostyrenes 3 underwent cycloaddition to afford the desired products 4 in excellent yields under solvent and metal free conditions. All the pyrrole derivatives were evaluated for their in vitro anti-bacterial activity. Among the synthesized pyrrole derivatives, 4b, 4c, 4e, 4g, 4i, 4j, 4l, 4m and 4n displayed good inhibitory properties against a panel of Gram positive and negative infectious pathogens.
机译:使用环境友好的碘催化的[3 + 2]环化反应,通过一种简单,快速且有效的方法合成了新型的高度取代的吡咯。对N-甲基-N-[((E)-1-(甲基硫烷基)-2-硝基-1-乙烯基]胺(NMSM)1和β-硝基苯乙烯3进行环加成反应,从而在溶剂和金属下以优异的收率得到所需的产物4免费条件。评价所有吡咯衍生物的体外抗菌活性。在合成的吡咯衍生物中,4b,4c,4e,4g,4i,4j,4l,4m和4n对一组革兰氏阳性和阴性传染病原体表现出良好的抑制特性。

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