| Abstract
| - Novel tricyclic pyrimido[4,5-b][1,4]benzothiazepines were readily prepared from 5-amino-4,6-bis(arylthio)pyrimidines and carboxylic acids via Bischler−Napieralski-type reactions. The 6-arylsulfide group of the resulting pyrimido[4,5-b][1,4]benzothiazepines could be selectively oxidized toits corresponding sulfoxide, which underwent facile substitution reactions when treated withnucleophiles such as an amine. This synthetic strategy provides an efficient way to access a libraryof novel heterocyclic compounds that are of interest in drug discovery.
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