One-Pot Sonogashira Coupling–Cyclization toward Regioselective Synthesis of Benzosultams

A one-pot
method for the Sonogashira coupling and cyclization of 2-bromobenzenesulfonamides
and terminal alkynes is presented. This method allows access to a
variety of substituted benzosultams regioselectively in excellent
yields. The reasons for regioselectivity are interpreted through density
functional theory (DFT) studies.

本方法提出了一种单步法，用于实现2-溴苯磺酰胺与末端炔烃的Sonogashira偶联和环化反应。该方法能够以区域选择性高、产率优异的特性，获得多种取代的苯磺脒衍生物。对于区域选择性的原因，通过密度泛函理论（DFT）研究进行了阐释。