Cordi A A, Lacoste J M, Le Borgne F, Herve Y, Vaysse-Ludot L, Descombes J J, Courchay C, Laubie M, Verbeuren T J
Institut de Recherches Servier, Suresnes, France.
J Med Chem. 1997 Aug 29;40(18):2931-5. doi: 10.1021/jm970282m.
Recently, we reported on the design, synthesis, and structure-activity relationships of a series of spiroimidazolines endowed with alpha-adrenergic agonist activities. Among the compounds described, (R,S)-spiro(1,3-diazacyclopent-1-ene)-[5,2'](7'-methyl-1'2',3', 4',-tetrahydronaphthalene) fumarate (5RS) was chosen for further development as a venotonic agent. The resolution of this compound, as well as the pharmacological characterization of the enantiomers, stereospecific synthesis of eutomer (5S, S 18149), and determination of absolute configuration by single-crystal X-ray diffraction analysis, are described.
最近，我们报道了一系列具有α-肾上腺素能激动剂活性的螺咪唑啉的设计、合成及构效关系。在所描述的化合物中，富马酸（R,S）-螺（1,3-二氮杂环戊-1-烯）-[5,2']（7'-甲基-1',2',3',4'-四氢萘）（5RS）被选作静脉张力调节剂进行进一步研发。本文描述了该化合物的拆分、对映体的药理学特性、优映体（5S,S 18149）的立体定向合成以及通过单晶X射线衍射分析确定绝对构型。
