Synthesis of novel 1-, 1,4- and 1,7-substituted 2-mercapto- and 2-methylmercapto- benzimidazoles: Acyclic analogues of the HIV-1 RT inhibitor, TIBO

John M. Gardiner, Colin R. Loyns

    Research output: Contribution to journalArticlepeer-review

    Abstract

    Synthetic approaches towards acyclic analogues of the HIV-1 RT inhibitor TIBO ring system, lacking either the diazepine C7 methylene, C5-N6 bond or the N1-N6 two-carbon bridge, are reported, utilizing ring opening reactions of 2-methylaziridines. A number of isomeric 2-methylmercaptobenzimidazole analogues have also been prepared, and the regiochemistry of 2-methylmercaptobenzimidazole alkylations is discussed, as a convenient route to 1,2,7-trifunctionalized benzimidazoles. © 1995 Elsevier Science Ltd, Printed in Great Britain. All rights reserved.
    Original languageEnglish
    Pages (from-to)11515-11530
    Number of pages15
    JournalTetrahedron
    Volume51
    Issue number42
    DOIs
    Publication statusPublished - 16 Oct 1995

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