非甾体抗生育药的研究 Ⅰ.对羟基苯丙烯酸及其类似物的合成

Studies On the Non-Steroidal Antifertility Agents Ⅰ. Synthesis of p-Coumaric Acid and Its Analogues

摘要: 1979年 A.Pakrashi 等自印度马兜铃(Aristolochia Indica L.)的根中分离得对-羟基苯丙烯酸和马兜铃次酸(Aristolic acid),经小鼠试验,证明对-羟基苯丙烯酸具有很好的抗生育活性,并认为其作用是在胚泡着床后中止妊娠的结果。为了验证其效果,我们先合成了该化合物,然后改变芳环上的取代基及其位置,用乙基取代а-位上的氢以及做成酯等制备了八个类似物，以观察对抗生育活性的影响。

Abstract: It was reported that p-coumaric acid showed 100% interceptive activity on day 6 preganant mice at the single oral dose of 50mg/kg of body weight. Thus p-coumaricacid and its eight analogues were synthesized for evaluation of their antifertilityefficacy. Preliminary pharmacological test indicated that p-coumaric acid and compoundⅢ、Ⅷ did not exhibit any antifertility activity in mice.