N-4′-(4″-羟基-苯甲酰氧基)-苯甲酰基-金刚烷甲酰肼的合成

摘要

通过对抗流感病毒药物的研究,希望获得抗病毒活性更强、选择性更好、毒副作用更小的金刚烷类似物.新合成的目标化合物可作为具有知识产权的抗病毒候选药物进一步开发研究,为研究用于临床的抗病毒药物奠定基础.由金刚烷甲酸合成金刚烷甲酸甲酯,再与水合肼反应,得到金刚烷甲酰肼,将金刚烷甲酰肼与对羟基苯甲酰氯反应制得目标化合物N-[4′-(4″-羟基-苯甲酰氧基)-苯甲酰基]-金刚烷甲酰肼.产物结构经ESI-MS测定,目标化合物结构正确.%Through the study of anti-influenza drugs,this work aims to gain stronger antiviral activity, better selectivity and less side effects of adamantane analogues.The new synthetic compounds can be used as antiviral candidate drugs with intellectual property,for further development research and for the study of clinical antiviral drugs.Adamantane methyl formate was synthesized by using adamantane formic acid and methanol as starting material,concentrated sulfuric acid as catalyst.Adamantane methyl formate reacted with hydrazine hydrate to obtain adamantane formyl hydrazine.The target compound N-[4′-(4″-hydroxyl-benzoyl oxygen group)-benzoyl group]-adamantane formyl hydrazine was produced when adamantane formyl hydrazine reacted with P-hydroxyl benzoyl chloride.The structure of target compound was deter-mined by ESI-MS.