【摘要】 为了寻找男用计划生育药物,本文报道睾丸酮十一烷酸酯的两种合成方法。(1)法睾丸酮(18g)溶于120ml无水苯及18g三乙胺的溶液中,搅拌下滴加18g十一烷酰氯,反应1小时;得到20.9g(73.2％)睾丸酮十一烷酸酯,熔点59～61℃,(2)法睾丸酮(7.2g),十一烷酸(6g),对甲苯磺酸(0.5g)悬浮于35ml无水苯中,搅拌下滴加5ml三氟乙酸酐,室温反应4～5小时,分离出固体用丙酮重结晶得6.95g(60.9％),物理常数与(1)法产物相同。药理试验结果表明TU与TP(丙睾)、TE(庚睾)比较具有较佳的活性与持久性,为一有希望的长效雄性激素。更多还原

【Abstract】 In searching for male contraceptives two methods of synthesis of testosterone undecanoate (TU) are described in the present article. Method (1) Testosterone (18g) was dissolved in a solution of 18g trie hylamine in 120 ml dry benzene, stirred with 18 g undecanoyl chloride for 1 hr. The residue gaTe 20.9g (73.3%) of TU. m.p.59～61C. Method (2) Trifluoroacetic anhydride (5ml) was added dropwise to a solution of testosterone (7.2g), undecanoic acid (6g)and p-toluene sulfonic acid (0.5g) in dry benzene (35ml), stirred for 4～5 hrs. at room temperature. The resulting solid crystal from acetone gave 6.95g(60.9％) of TU. The physical constants of the product were in agreement with those of Method (1). pharmacological results showfd that TU is a hopeful long-acting androgenic hormone with the best activity and longest duration in comparison with testosttrone propionate (TP) and testosterone enanthste(TE).更多还原