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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。
In order to find male family planning drugs, this article reports two methods of synthesizing testosterone undecanoate. (1) Method Testosterone (18 g) was dissolved in 120 ml of anhydrous benzene and 18 g of triethylamine, and 18 g of undecanoyl chloride was added dropwise thereto under stirring for 1 hour; 20.9 g (73.2%) of testosterone undecanoate , Melting point 59 to 61 ° C, testosterone (7.2g), undecanoic acid (6g) and p-toluenesulfonic acid (0.5g) were suspended in 35ml of dry benzene under the conditions of (2), and 5ml of trifluoroacetic anhydride , The reaction was carried out at room temperature for 4 to 5 hours, and the solid separated out was recrystallized from acetone to obtain 6.95 g (60.9%). The physical constants were the same as those of the product of (1). Pharmacological test results show that TU and TP (testis), TE (heptylserum) compared with better activity and durability, as a promising long-acting androgen.