【摘要】 为寻求更有效的避孕药,合成了九个双炔失碳酯(Ⅰ)的类似物。其中七个类似物目前尚未见文献报道。本文给出这些化合物的合成方法,红外光谱及质谱数据,并讨论了合成中遇到的一些问题。这些化合物对小白鼠的抗早孕和抗着床的初步试验结果,化合物X的抗早孕效果优于化合物Ⅰ。更多还原

【Abstract】 In order to obtain effective contraceptives, nine anordrin (I) analogs were synthesized by esterification of compound (Ⅱ) with several methods, such as PTSanhydride (Ⅲ, Ⅳ, Ⅴ, Ⅸ) Pyridine-acylchloride (Ⅵ-Ⅷ) and direct esterification by the catalysis of DCC-DMAF (Ⅺ). TFA method was also tried for preparing compound (Ⅸ). Seven of these compounds. (Ⅳ-Ⅸ, Ⅺ) have not been found to the literature. Their structures were determined by IR-spectrum, mass spectrum and elementai analysis. Some questions were discussed in the synthesis. Preliminary test for anti-early pregnancy and anti-implantation in mice of these compounds were determined, the effect of anti-early pregnancy of comppund X is more active than compound I更多还原