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Synlett 2008(3): 418-422  
DOI: 10.1055/s-2008-1032064
LETTER
© Georg Thieme Verlag Stuttgart · New York

A Chemobiological Synthesis of Eplerenone

Peter G. M. Wuts*, Andrew M. Anderson, Scott W. Ashford, Michael P. Goble, Michael J. White, Doris Beck, Ivan Gilbert, R. E. Hrab
Pfizer Global Research and Development, Groton, CT 06340 and Pfizer, Bioprocess Development Group, Kalamazoo, MI 49001, USA
Fax: +1(860)4410599; e-Mail: peter.g.wuts@pfizer.com;
Further Information

Publication History

Received 12 November 2007
Publication Date:
23 January 2008 (online)

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Abstract

This paper will describe an approach to the synthesis of eplerenone, which is being marketed for the treatment of hypertension. The synthesis begins with DHEA available from wild yams and uses a combination of microbiological and chemical transformations to build eplerenone.

Key words

carbonylation - microbial oxidation - hydroformylation - steroids - Ishikawa reagent - microbial deprotection

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Mackey, S. S.; Matison, M. E.; Wu, H. unpublished results.