Hosztafi S, Köhegyi I, Simon C, Fürst Z
Alkaloida Chemical Company Ltd., Tiszavasvári, Hungary.
Arzneimittelforschung. 1993 Nov;43(11):1200-3.
The synthesis of morphine nicotinates is described using nicotinyl chloride in the presence of pyridine. Isomorphine and isocodeine nicotinates were prepared from the corresponding morphine and codeine derivatives with nicotinic acid in the presence of triphenylphosphine and diethyl azodicarboxylate. Unexpectedly the reaction of 14-hydroxy-dihydromorphinone derivatives was anomalous, enolesters were formed. The analgetic activity of selected compounds was determined.
描述了在吡啶存在下使用烟酰氯合成吗啡烟酸盐的方法。异吗啡和异可待因烟酸盐是由相应的吗啡和可待因衍生物与烟酸在三苯基膦和偶氮二羧酸二乙酯存在下制备的。出乎意料的是,14-羟基二氢吗啡酮衍生物的反应异常,形成了烯醇酯。测定了所选化合物的镇痛活性。