Modification of the parent structure of molecules often alters their physicochemical properties and biological activities. Herein, a practical, efficient, and highly regioselective C–H alkylation of phenols with alcohols via dehydroxylative cross-coupling was developed to produce para-alkylated phenols with excellent regioselectivities and yields, using which propofol derivatives were rapidly synthesized
分子母体结构的修饰通常会改变其理化性质和
生物活性。在此,开发了一种实用、高效、高度区域选择性的
苯酚与醇通过脱羟基交叉偶联的C-H烷基化反应,以生产具有优异区域选择性和产率的对烷基化
苯酚,并利用该方法快速合成
丙泊酚衍
生物。该过程在温和、简单的条件下进行,并且与多种醇(仲、叔
苄醇以及
烯丙醇)作为烷基化剂具有良好的相容性。此外,利用该催化体系还得到了高芳基醚衍
生物。