申请人:——
公开号:US04016289A1
公开(公告)日:1977-04-05
A medicinal preparation for treatment of viral-etiology diseases contains the bisulphite compound of 2-fluorenonyl-glyoxal in combination with a pharmaceutical vehicle or unctuous base. A method of producing the bisulphite compound of 2-fluorenonyl-glyoxal, viz, the active principle of said medicinal preparation, consists in that fluorene is acylated by dichloroacetyl chloride in the presence of aluminum chloride and phosphoryl chloride in an organic solvent, the resultant 2-.omega.-dichloroacetylfluorene is oxidized by the salts of chromic acid in an acetic-acid medium at 50.degree.-90.degree. C into 2-.omega.-dichloroacetylfluorenone which is made to interact with morpholine at 50.degree.-98.degree. C to form 2-.omega.-dimorpholinoacetylflourenone, or otherwise, fluorenone is acylated by acetic anhydride in an organic solvent in the presence of aluminum chloride, the resultant 2-acetylfluorene is oxidized by chromic acid or by the salts thereof in an acetic acid medium at 50.degree.-90.degree. C to obtain 2-acetylfluorenone which is brominated in an organic solvent at 60.degree.-110.degree. C, the resultant 2-.omega.-dibromoacetylfluorenone is reacted with morpholine at 50.degree.-98.degree. C to form 2-.omega.-dimorpholinoacetylfluorenone the latter is hydrolyzed by dilute mineral acids at 20.degree.-100.degree. C into 2-fluorenonyl-glyoxal hydrate which is then made to react with sodium bisulphite in an aqueous-alcohol medium at 60.degree.-80.degree. C to isolate the final product.
治疗病毒性疾病的药物制剂包含2-氟萘基-乙二醛的亚硫酸盐化合物,与药用载体或油脂基相结合。生产2-氟萘基-乙二醛的亚硫酸盐化合物的方法,即所述药物制剂的活性成分,包括在有机溶剂中,通过氯化二氯乙酰氯在铝氯化物和磷酰氯的存在下对氟烯进行酰化,得到的2-ω-二氯乙酰基氟烯经由醋酸介质中的铬酸盐氧化在50°C-90°C条件下转化为2-ω-二氯乙酰基氟醌,然后与吗啡啶在50°C-98°C反应形成2-ω-二吗啡啶基乙酰氟醌,或者,氟醌通过醋酸酐在有机溶剂中在铝氯化物的存在下酰化,得到的2-乙酰基氟醌经由铬酸或其盐在醋酸介质中在50°C-90°C条件下氧化得到2-乙酰基氟醌,然后在有机溶剂中在60°C-110°C条件下溴化,得到的2-ω-二溴乙酰基氟醌与吗啡啶在50°C-98°C反应形成2-ω-二吗啡啶基乙酰氟醌,后者通过稀释的矿酸在20°C-100°C条件下水解为2-氟萘基-乙二醛水合物,然后与硫代亚砜钠在60°C-80°C条件下在水-醇介质中反应以分离最终产物。