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在控制生育的药物分子中引入三芳基乙烯或乙烷和二烷胺基乙氧基侧链的重要性业已肯定。最近在研究二苯基-苯丙烯酮、二苯基-苯丙酮及二苯丙烯类过程中发现赤型2,3-二苯基-4′-(β-四氢吡咯乙氧基)苯戊酮(Ⅰ)为极有效的抗生育药物。后又合成了22～41一系列化合物,其中除变换2,3,4′位的取代基以适应抗生育的结构要求外,分子骨架与I类似。本文介绍用羟基酮为原料制备2,3-双取代4′(β-二烷胺基乙氧基)苯丙酮(32～41)的合成路线以及抗生育活性的构-效关系。
The importance of introducing triarylethene or ethane and dialkylaminoethoxy side chains in fertile drug molecules has been confirmed. Recently in the study of diphenyl-phenylpropenone, diphenylpropiophenone and diphenylpropylene class found in the process of erythro-2,3-diphenyl-4 ’- (β-tetrahydropyrrole ethoxy) Ketone (I) is a very effective anti-fertility drug. Later, a series of compounds from 22 to 41 were synthesized, in which the molecular framework was similar to I except that the substituents at 2,3,4 ’were changed to meet the structural requirements of anti-fertility. In this paper, the synthetic route of 2,3-disubstituted 4 ’(β-dialkylaminoethoxy) propiophenone (32-41) and the structure-activity relationship of its anti-fertility activity using hydroxyketones as raw materials are introduced.