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Synfacts 2010(4): 0384-0384  
DOI: 10.1055/s-0029-1219485
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of the Benzimidazole Fragment of BYK405879

Contributor(s): Philip Kocienski
M. Webel*, A. M. Palmer*, C. Scheufler, D. Haag, B. Müller
NYCOMED, Konstanz and Singen, Germany
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Publication History

Publication Date:
22 March 2010 (online)

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Significance

BYK405879 is a reversible inhibitor of the gastric proton pump enzyme that is a lead treatment for gastroesophageal reflux disease. This paper describes a shorter and more efficient large-scale synthesis of the late-stage benzimid­azole intermediate G en route to BYK405879 (A. M. Palmer et al. Org. Process Res. Dev. 2008, 12, 1170).