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双炔失碳酯、1,8-双二氯乙酰辛二胺(又称Win 18446)是两种避孕药物,前者为女用避孕药,后者能抑制生精过程,是有希望的男性抗生育药物。为了研究它们在体内的吸收分布和代谢以指导合理用药。我们合成了它们的~(14)C-标记化合物。双炔失碳酯(Ⅰ)的标记其合成路线基本与非标记合成相似,但操作上作了适当改进。所用乙炔-~(14)C_2,是用碳酸钡-~(14)C(0.5g,5mCi)按文献方法制备。 我们用1,6-二溴己烷与氰化钾-~(14)C作用成相应的二腈化合物(Ⅴ),经还原成1,8-二氨基辛烷-1,8-~(14)C_2(Ⅵ),再与二氯乙酸乙酯反应即得~(14)C-标记的Ⅱ。反应式如下:
Anordrin, 1,8-Dichloroacetic acid (also known as Win 18446) is two contraceptives, the former female contraceptives, the latter can inhibit the process of spermatogenesis, there is hope that the male anti- Fertility medicine. In order to study their absorption distribution in the body and metabolism to guide the rational use of drugs. We synthesized their ~ (14) C-labeled compounds. The procedure for the synthesis of the anilthrin (I) was similar to that of the unlabeled synthesis, but was appropriately modified in terms of its operation. Acetylene- ~ (14) C_2 was prepared by literature method using barium carbonate ~ (14) C (0.5g, 5mCi). We used 1,6-dibromohexane with potassium cyanide - ~ (14) C to form the corresponding dinitrile compound (V), which was reduced to 1,8-diaminooctane-1,8- ) C_2 (Ⅵ) and react with dichloroacetate to obtain ~ (14) C-labeled Ⅱ. The reaction is as follows: