UC84及其衍生物的合成

Synthesis of UC 84 and Its Derivatives

合成了化合物 2 氯 5 (5 ,6 二氢 2 甲基 1,4 氧硫杂环己二烯 3 甲酰氨基 )苯甲酸异丙酯(UC 84) ,并以其为先导物合成了 11个未见报道的衍生物 ,活性筛选表明该类化合物有明显的抗单纯疱疹病毒 (HSV)和乙肝病毒 (HBV)

Methylethyl 2 chloro 5 〔〔(5,6 dihydro 2 methyl 1,4 oxathiin 3 yl)carbonyl〕amino〕benzoate(UC 84) has the strong anti HIV activity which was found by Bader in National Cancer Institute,National Institute of Health in 1991 while screening for anti AIDS compounds.Its simple structure and obvious activity made us synthesize a series of derivatives seeking for a potential anti HBV and anti HSV compounds.According to the structure of UC 84,5,6 dihydro 2 methyl 1,4 oxathiin 3 carbonyl chloride(4) was treated with various amino compounds and 11 derivatives of UC 84 were obtained.All these compounds were evaluated,and some of them showed obvious anti HSV and anti HBV activities.The results indicated that the derivatives of 1 methylethyl 2 chloro 5 〔〔(5,6 dihydro 2 methyl 1,4 oxathiin 3 yl)carbonyl〕amino〕benzoate(UC 84) might be the potential anti HSV and anti HBV drugs in future.