铜催化溴化苄与磺酰肼的偶联反应合成砜类化合物

Copper-catalyzed coupling reaction of benzyl bromide with sulfonyl hydrazide for synthesis of sulfone compounds

  • 摘要: 砜类化合物广泛存在于药物和精细化学品中,由于砜骨架的存在,其在生物化学、药物化学和有机合成中具有重要的应用. 该论文通过研究发现了一种溴化苄与磺酰肼偶联制备砜类化合物的方法,以CuI为催化剂,TBHP为氧化剂,K2CO3为碱,在室温条件下反应生成偶联产物砜,产率最高可达85%. 该方法具有底物适用性好、收率良好至优秀、反应条件温和等特点,为砜类化合物的合成提供了一种新的方法. 通过该方法合成了24个砜类化合物,产物结构均经过1H NMR和13C NMR表征.

     

    Abstract: Sulfone compounds are found in a wide range of drugs and fine chemicals and have important applications in biochemistry, medicinal chemistry and organic synthesis due to the presence of sulfone skeleton. In this paper, a method for the preparation of sulfone compounds by coupling benzyl bromide with sulfonylhydrazine has been found to produce the coupling product sulfone in yields up to 85% by reaction at room temperature using CuI as catalyst, TBHP as oxidant and K2CO3 as base. The method is characterized by good substrate suitability, good to excellent yields and mild reaction conditions, providing a new method for the synthesis of sulfone compounds. Twenty-four sulfone compounds were synthesized by the method and the product structures were characterized by 1H NMR and 13C NMR.

     

/

返回文章
返回