论文部分内容阅读
目的合成一系列含二茂铁基的Schiff碱类化合物,并测定其体外抗真菌活性。方法以二茂铁为起始原料,经乙酰化、氧化、酰化、肼解制得中间体二茂铁甲酰肼(1);以各种4-取代的苯硫酚和3-氯丙酸为起始原料,经取代、环合制得中间体取代2H-苯并[b]噻喃-4-酮(2a);以取代苯酚和3-氯丙酸为起始原料,经加成、环合制得中间体取代2H-苯并[b]吡喃-4-酮(2b);以各种取代苯胺和丙烯酸为起始原料,经加成、环合制得中间体取代2,3-二氢喹啉-4(1H)-酮(2c),中间体2a、2b、2c分别与1反应得到目标化合物。采用二倍浓度稀释法测试各目标化合物的体外抗真菌活性。结果与结论合成的15个化合物均未见文献报道,其结构经1H-NM R、HRM S谱确证;活性测试结果表明,多个目标化合物对测试真菌表现出一定的体外抑菌活性。
AIM: To synthesize a series of Schiff bases containing ferrocenyl groups and determine their antifungal activity in vitro. Methods Ferrocene was used as the starting material to obtain the intermediate ferrocene hydrazide (1) via acetylation, oxidation, acylation and hydrazinolysis. The intermediate 4-substituted thiophenol and 3-chloropropionic acid As the starting material, the intermediate substituted 2H-benzo [b] thiopyran-4-one (2a) was obtained by substitution and cyclization; the substituted phenol and 3-chloropropionic acid were used as starting materials, Cyclodehydration intermediates prepared 2H-benzo [b] pyran-4-one (2b); various substituted anilines and acrylic acid as the starting material, through addition, cyclization intermediates were substituted 2,3 - dihydroquinolin-4 (1H) -one (2c), intermediates 2a, 2b, 2c, respectively, were reacted with 1 to afford the title compound. In vitro antifungal activity of each of the target compounds was tested using a double dilution method. RESULTS AND CONCLUSION None of the 15 compounds synthesized were reported in the literature. Their structures were confirmed by 1H-NM R and HRM S spectra. The results of the activity test showed that many of the target compounds showed some antibacterial activities against the tested fungi.