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本文介绍用α-萘乙酸乙酯与相应的格氏试剂反应,继以酸催化脱水,得三芳基取代乙烯,然后用卤素、硝酸等处理,合成了十七个1,1-二苯基萘乙烯类化合物。所有化合物对大白鼠或家兔进行抗生育试验,发现化合物6931,70082,70083,在10mg/kg/天剂量下,口服六天,对大白鼠有100%的抗生育效果。其中化合物6931在5mg/kg/天剂量下,口服三天能完全抑制家兔生育。当分子中乙烯氢原子被卤素及硝基取代后,抗生育效果显著下降。
In this paper, the reaction of ethyl α-naphthylacetate with the corresponding Grignard reagent followed by acid-catalyzed dehydration gave the triaryl-substituted ethylene followed by treatment with halogen, nitric acid and the like to synthesize seventeen 1,1-diphenylnaphthalene Ethylene compounds. All compounds were tested for antifertility in rats or in rats and found that compounds 6931, 70082, 70083 were orally administered for 6 days at a dose of 10 mg / kg / day and had a 100% antibiotic effect on rats. Among them, compound 6931 could completely inhibit the birth of rabbits at the dose of 5mg / kg / day for three days. When the molecules of ethylene hydrogen atoms were replaced by halogen and nitro, the anti-fertility significantly reduced.