【摘要】 <正> 为了研究长效口服避孕药复方炔雌醚的作用机理,我们采用放射免疫测定法,测定服药者血中炔雌醚(17α-乙炔雌二醇-3-环戊醚)及其代谢产物炔雌醇(17α-乙炔雌二醇)的浓度,以观察它们的动态变化规律。甾体化合物的分子量较小,本身没有抗原性,所以须先制备半抗原,然后再与大分子载体,如牛血清白蛋白结合,方能使动物免疫而产生抗血清。目前甾体雌激素的半抗原多采用6-(O-羧甲基)肟衍生物。通常先用铬酐-乙酸氧化雌激素,引入6-酮基,再制成肟衍生物。但是铬酐-乙酸的氧化产物甚为复杂,得率亦低。我们采用Hofmeister的方法,将炔诺酮(1)用氧气氧化成炔雌醇6-酮(2a),然后再与溴代环戊烷反应,生成炔雌醚-6-酮(2b),化合物2a,2b分别与羧甲基羟胺半盐酸盐反应,生成相应的炔雌醇-更多还原

【Abstract】 A synthesis of the haptens of the long acting oral contraceptive quinestrol and its metabolic product ethynylestradiol has been described.Norlutin was used as the starting material and oxidized according to the method of Hofmeister to yeild the 6-oxo-ethynylestradiol, which was then reacted with cyclopentyl bromide to give the 6-oxo-qninestrol. Both 6-oxo-ethynylestradiol and 6-oxoquinestrol were then reacted respectively with carboxy-methoxylamine hemihydrochloride to give the corresponding 6-(O-carboxymethyl) oxime derivatives of 6-oxoquinestrol and 6-oxo-ethynylestradiol.更多还原