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Formation of N-heterocycles by the reaction of thiols with glyoxamides: exploring a connective Pummerer-type cyclisation†
Marc Miller,Johannes C. Vogel,William Tsang,Andrew Merrit,David J. Procter
Organic & Biomolecular Chemistry Pub Date : 12/12/2008 00:00:00 , DOI:10.1039/B816608K
Abstract

The reaction of thiols with glyoxamides provides a convenient method for the generation of thionium ions and the initiation of Pummerer-type reactions. When the glyoxamides contain tethered aromatic nucleophiles, N-heterocycles are formed by a thionium ion cyclisation. The scope and mechanism of the connective Pummerer-type process has been investigated using a range of thiols, Lewis acids and both mono- and bis-glyoxamides. The utility of the process has been illustrated in a synthesis of the indoloquinoline natural product, neocryptolepine.

Graphical abstract: Formation of N-heterocycles by the reaction of thiols with glyoxamides: exploring a connective Pummerer-type cyclisation
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