Synthesis of MK-8141

D. Gauvreau; G. J. Hughes; S. Y. W. Lau; D. J. McKay; P. D. O’Shea; R. R. Sidler; B. Yu; I. W. Davies

doi:10.1055/s-0030-1259211

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Synfacts 2011(2): 0120-0120
DOI: 10.1055/s-0030-1259211

Synthesis of Natural Products and Potential Drugs

Synthesis of MK-8141

Contributor(s): Philip Kocienski
D. Gauvreau*, G. J. Hughes, S. Y. W. Lau, D. J. McKay, P. D. O’Shea, R. R. Sidler, B. Yu, I. W. Davies
Merck Frosst, Kirkland, Canada

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Publication History

Publication Date:
19 January 2011 (online)

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Significance

MK-8141 inhibits renin, an aspartyl protease that is targeted for the regulation of high blood pressure and heart failure. The synthesis of MK-8141 features a diastereoselective Dieckmann cyclization of the diester C to give the 3,9-diazabicyclo-[3.3.1]nonenes D and E (1:8.5).