✦ LIBER ✦

Liquid-phase synthesis of 2-(alkylthio) benzimidazoles

✍ Scribed by Chih-Ming Yeh; Chung-Ming Sun

Publisher: Elsevier Science
Year: 1999
Tongue: French
Weight: 244 KB
Volume: 40
Category: Article
ISSN: 0040-4039
DOI: 10.1016/s0040-4039(99)01487-2

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✦ Synopsis

An efficient liquid-phase synthesis of 2-alkylthio-5-carbamoylbenzimidazoles 1 is described. Immobilized ofluoronitrobenzene 2 undergoes nucleophilic addition of primary amine to afford o-nitroaniline derivatives 3. Subsequent reduction of the aromatic nitro group followed by cyclization gives a PEG-bound benzimidazole-2thione 5. S-Alkylation of polymer-supported scaffold 5 followed by cleavage gives the resulting library in high yield and high purity.

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