Abstract
An efficient liquid-phase synthesis of 2-alkylthio-5-carbamoylbenzimidazoles 1 is described. Immobilized o-fluoronitrobenzene 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-2-thione 5. S-Alkylation of polymer-supported scaffold 5 followed by cleavage gives the resulting library in high yield and high purity.
Original language | English |
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Pages (from-to) | 7247-7250 |
Number of pages | 4 |
Journal | Tetrahedron Letters |
Volume | 40 |
Issue number | 40 |
DOIs | |
State | Published - 1 Oct 1999 |