In the present investigation, the first construction of a series of structurally new 2‐ferrocenoyl‐substituted iodobenzofurans hybrids has been achieved through a simple and mild two‐step procedure, involving the iodination of salicylaldehydes using N‐iodosuccinimide reagent in eco‐friendly PEG‐400 medium at room temperature followed by one‐pot Rap–Stoermer reaction with 1‐chloroacetylferrocene in refluxing MeCN with the presence of K2CO3 as base and PEG‐400 as the activated additive. These newly synthesized compounds belong to a new class of ferrocene‐benzofuran hybrids and could be good candidates for the development of compounds for use in medicinal chemistry.
The incorporation of the 3-methylbenzofuran moiety into the ferrocene nucleus leading to a series of structurally novel hybrids 2-ferrocenoyl-3-methylbenzofuran derivatives has been achieved in good yields of 76-85% through the one-pot Rap-Stoermer reaction of 1-chloroacetylferrocene with 2′-hydroxyacetophenones in refluxing CH 3 CN with the presence of K 2 CO 3 as base and PEG-400 as catalyst. These newly-synthesised compounds could be good candidates for the development of compounds for use in medicinal chemistry.
An efficient and easy method for the synthesis of thiazole-containing indole derivatives was described, involving the condensation reaction of 5-chloroacetyloxindole with thiourea (substituted thiourea) and thioamide in the solvent of absolute ethanol via Hantzseh reaction to give the corresponding 5-(2-substituted-thiazol-4-yl)indolin-2-one (2a~2k) and 5-(2-substituted-thiazol-4-yl)indolin-2-one (2l~2q), respectively. The procedure has the advantages of simple operation, mild reaction conditions, and good yields. All of compounds were new and their structures were confirmed by IR, MS, P 1 P H NMR and P 13 P C NMR spectra and elemental analyses. Keywords 5-chloroacetyloxindole; thioamide; thiourea; thiazole-containing; indole derivatives; synthesis 噻唑是一类含氮硫杂原子的五元芳杂环, 这种结构 赋予了噻唑类化合物诸多特殊的性能, 在众多领域具有 广泛的潜在应用, 引起化学工作者和药学家的极大关 注 [1,2] . 在医药领域, 噻唑类化合物表现出抗细菌 [3] 、抗 病毒 [4] 、抗癌 [5] 、抗结核 [6] 、消炎镇痛 [7] 和抗寄生虫 [8] 等 多种生物活性; 在农业领域, 噻唑类化合物作为良好的 除草剂 [9] 、植物生长调节剂 [10] 以及杀菌和杀虫剂 [11~13]
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