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Synlett 1999; 1999(6): 810-812
DOI: 10.1055/s-1999-2739
DOI: 10.1055/s-1999-2739
letter
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Rapid Parallel Synthesis of Benzimidazoles
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Publikationsverlauf
Publikationsdatum:
31. Dezember 1999 (online)
Soluble polymer-supported solution synthesis of 2-alkylthiobenzimidazoles 1 has been developed. Treatment of polymer bound o-fluoronitrobenzene 2 with various primary amines affords o-nitroaniline derivatives. Reduction of the aromatic nitro group followed by cyclization gives a benzimidazole-2-thione 5. Reaction of 5 with alkyl halides followed by cleavage provides final compounds in high yield and high purity after six steps.
benzimidazole - combinatorial chemistry - liquid-phase method - solid-phase method - scaffold