醋炔诺酮肟是新的避孕药物,其抗着床作用为炔诺酮的12.5倍。为研究它在体内药代动力学模型与过程,用多步有机反应合成了四个氚标记系列避孕药物:[6,7-~3H]炔诺醋(Ⅱ)、[6,7-~3H]醋炔诺酮(Ⅲ)、[6,7-~3H]炔诺酮肟(Ⅳ)和[6,7-~3H]醋炔诺酮肟(Ⅴ)。此外,还通过催化氚化还原反应合成了中间体[6,7-~3H]19-去甲基-4-雄烯-3,17-二酮(Ⅰ)和炔锂乙二胺络合物(固体)。 Acetoxynil oxime is a new contraceptive that has 12.5 times the anti-implantation effect as norethindrone. In order to study its pharmacokinetic model and process in vivo, four series of tritium labeled contraceptives were synthesized by multi-step organic reactions: [6,7- ~ 3H] ninoreasate (Ⅱ), [6,7- ~ 3H ] Norethindrone acetate (III), [6,7- ~ 3H] norethindrone oxime (IV) and [6,7- ~ 3H] acetoxynil oxime (V). In addition, the intermediate [6,7- ~ 3H] 19-nor-methyl-4-androstene-3,17-dione (Ⅰ) and alkyne lithium ethylenediamine complex were also synthesized by catalytic tritium reduction (solid).