An efficient andc onvenient synthesis of pyrrolo[1,2-a]quinoxalines from 1-(2-aminoaryl)pyrrole anda rylacetic acids has been described by using acombination of CuSO 4 as the catalysta nd 2,2'-bipyridyl ast he ligand in the presence of O 2 as an oxidant. The prominentf eatures of this method are the use of readily availablestarting materials, inexpensive catalyst, broad substrate scope and high product yields.
A metal-free and efficient tandem synthesis of 3-acyl 3,4-dihydro-2H-1,2,4-benzothiadiazine-1,1-dioxides and 3-acyl-2H-1,2,4-benzothiadiazine-1,1-dioxides has been developed via CÀH functionalization of ethynylarenes and ethenylarenes followed by condensation with 2-aminobenzenesulfonamide. The reaction involves the formation of arylglyoxal as an intermediate from multiform substrates through Kornblum oxidation in the presence of iodine and DMSO. Use of simple and readily available starting materials, inexpensive reagent, broad substrate scope and a very simple operation are noteworthy features of this protocol. This method provides an easy access to pharmaceutically important 3-acyl-1,2,4-benzothiadiazine-1,1-dioxides in good yields.
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