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本文报道利用睾丸酮为原料,经脱氢和二甲基铜锂试剂甲基化,制备7-甲基睾丸酮。采用结晶法分离7α-和7β-异构体后,分别进行锂氨还原、氧化、环合及炔锂炔化等反应,合成7α-和7β-甲基-A-环失碳-2α,17α-双乙炔基-5α-雄甾-2β,17β-二醇(Ⅱa,和Ⅱb),经初步药理试验表明,Ⅱa对大鼠具有较强的抗孕激素活性,口服剂量在2.5 mg/kg时,能明显抑制假孕大鼠蜕膜瘤的生长。抗早孕最低口服有效剂量为3.5 mg/kg/4 d,Ⅱb则较弱。
This paper reports the use of testosterone as raw material, dehydrogenation and dimethyl-copper-lithium reagent methylation, preparation of 7-methyl testosterone. The 7α- and 7β-isomers were separated by crystallization, and then the reactions of lithium reduction, oxidation, cyclization and alkyne lithium were carried out separately to synthesize 7α- and 7β-methyl-A-ring carbon-2α, 17α -ethylenyl-5α-androsta-2β, 17β-diol (Ⅱa and Ⅱb). The results of preliminary pharmacological experiments showed that Ⅱa had strong antiprogestin activity in rats. When the oral dose was 2.5 mg / kg , Can significantly inhibit the growth of decidua in pseudopregnant rats. The lowest oral effective dose of anti-pregnancy pregnancy was 3.5 mg / kg / 4 d, Ⅱ b is weaker.