el-Ablack Fawzia Zakeria
Chemistry Department, Damietta Faculty of Science, Mansoura University, Egypt.
Boll Chim Farm. 2003 Nov;142(9):406-9.
Reaction of 4-amino-3-phenyl-5-ethoxycarbonyl-thiazole-2-thione with phenylisothiocyanate gave (2) which when boiled with acetic acid gave (3). Treatment of (2) with monochloroacetic acid resulted in the formation of thiazolidinone derivative (4). Reaction of (2) with malonic acid gave (5). Condensation of (1) with aromatic aldehydes afforded Schiffe base derivatives (6a,b). Treatment of (1) with malononitrile, ethyl cyanoacetate and acetonitrile resulted the formation of pyridine derivatives (7a,b,c). The reaction of (1) with urea and thiourea gave compound (8). Condensation of (1) with o-phenylenediamine and o-aminophenol gave compound (9). Reaction of (1) with nitrous acid followed by coupling with ethylacetoacetate afforded (10). Bromination of (10) gave bromo derivative (11). The structures of the hitherto unknown compounds have been confirmed by analytical and spectral methods. The newly synthesized compounds were screened for antibacterial activity.
4-氨基-3-苯基-5-乙氧羰基噻唑-2-硫酮与苯基异硫氰酸酯反应生成(2)，(2)与乙酸煮沸后生成(3)。用一氯乙酸处理(2)得到噻唑烷酮衍生物(4)。(2)与丙二酸反应生成(5)。(1)与芳香醛缩合得到席夫碱衍生物(6a,b)。用丙二腈、氰基乙酸乙酯和乙腈处理(1)生成吡啶衍生物(7a,b,c)。(1)与尿素和硫脲反应生成化合物(8)。(1)与邻苯二胺和邻氨基酚缩合得到化合物(9)。(1)与亚硝酸反应，然后与乙酰乙酸乙酯偶联得到(10)。(10)溴化得到溴代衍生物(11)。迄今未知化合物的结构已通过分析和光谱方法得到证实。对新合成的化合物进行了抗菌活性筛选。
