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    • 4. 发明授权
    • Synthesis of cyclic disulfone compounds
    • 环状二砜化合物的合成
    • US4348529A
    • 1982-09-07
    • US294408
    • 1981-08-19
    • Alan L. BorrorErnest W. EllisCharles E. Hammond
    • Alan L. BorrorErnest W. EllisCharles E. Hammond
    • C07D339/08C07D339/00C07D339/06
    • C07D339/08
    • This invention relates to a method of synthesizing bis-sulfones of the formula ##STR1## wherein R.sup.1 and R.sup.2 each are hydrogen, alkyl, phenalkyl, phenyl or phenyl-substituted with an electron-donating or electron-withdrawing group and n is an integer 2, 3 or 4 (a) by reacting a 1,3-dithio compound with n-butyllithium to generate the anion of said compound, (b) reacting said anion with a carbonyl compound to give the 2-substituted carbonol anion intermediate, (c) reacting said intermediate with an acyl chloride or a chloroformate to give the corresponding ester, and (d) reacting said ester with a peracid to give the bis-sulfone product. The subject invention also is concerned with the novel intermediates of step (c).
    • 本发明涉及一种合成下式的双砜的方法,其中R 1和R 2各自为氢,烷基,苯烷基,苯基或被供电子基团或吸电子基团苯基取代,n为整数2 ,3或4(a)通过使1,3-二硫代化合物与正丁基锂反应以产生所述化合物的阴离子,(b)使所述阴离子与羰基化合物反应,得到2-取代的碳醇阴离子中间体,(c )使所述中间体与酰氯或氯甲酸酯反应,得到相应的酯,和(d)使所述酯与过酸反应,得到双砜产物。 本发明还涉及步骤(c)的新型中间体。