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Novel benzothiazole containing 4H-pyrimido[2,1-b]benzothiazoles derivatives: One pot, solvent-free microwave assisted synthesis and their biological evaluation
Arabian Journal of Chemistry ( IF 5.3 ) Pub Date : 2019-12-01 , DOI: 10.1016/j.arabjc.2016.01.012
Manoj N. Bhoi , Mayuri A. Borad , Edwin A. Pithawala , Hitesh D. Patel

Abstract Synthesis of new and desired compounds has an everlasting demand. The present work emphasizes on the one pot, three component microwave assisted synthesis of novel ethyl 2-methyl-4-(pyridin-2-yl)-4H-benzo[4,5]thiazolo[3,2-a]pyrimidine-3-carboxylate derivatives by the reaction of 2-aminobenzothiazole derivatives with Pyridine 2-aldehyde and Ethyl acetoacetate in the presence of PdCl2 as an expeditious catalyst under solvent-free condition. The salient features of this approach are operational simplicity, convergence, short reaction time, high atom economy, easy workup, mild reaction conditions and environmentally benign conditions. All the newly synthesized diverse poly-functionalized tri-heterocyclic benzothiazole derivatives have been characterized by elemental analysis and various spectroscopic methods such as FT-IR, 1H NMR, 13C NMR, ESI-MS and Single crystal X-ray analysis (4a). All the final scaffolds have been screened for antibacterial and antioxidant activities. Also their antitubercular activity against Mycobacterium tuberculosis H37RV was screened.

中文翻译:

含有 4H-嘧啶并[2,1-b]苯并噻唑衍生物的新型苯并噻唑:一锅无溶剂微波辅助合成及其生物学评价

摘要 合成新的和所需的化合物具有永恒的需求。目前的工作重点是一锅三组分微波辅助合成新型乙基2-甲基-4-(吡啶-2-基)-4H-苯并[4,5]噻唑并[3,2-a]嘧啶-3在无溶剂条件下,在作为快速催化剂的 PdCl2 存在下,2-氨基苯并噻唑衍生物与吡啶 2-醛和乙酰乙酸乙酯反应生成-羧酸衍生物。这种方法的显着特点是操作简单、收敛、反应时间短、原子经济性高、后处理容易、反应条件温和、环境友好。所有新合成的各种多官能化三杂环苯并噻唑衍生物均已通过元素分析和各种光谱方法(如 FT-IR、1H NMR、13C NMR、ESI-MS 和单晶 X 射线分析 (4a)。所有最终的支架都经过了抗菌和抗氧化活性的筛选。还筛选了它们对结核分枝杆菌 H37RV 的抗结核活性。
更新日期:2019-12-01
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