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Synfacts 2011(4): 0350-0350  
DOI: 10.1055/s-0030-1259591
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of the HIV Integrase Inhibitor Raltegravir Potassium

Contributor(s): Philip Kocienski
G. R. Humphrey*, P. J. Pye*, Y.-L. Zhong et al.*
Merck Research Laboratories, Rahway, USA
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Publication History

Publication Date:
18 March 2011 (online)

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Significance

Raltegravir (Isentress®) is an HIV integrase inhibitor prescribed for treating or prophylaxis of HIV infection and for delaying the onset of AIDS. It is a first-in-class drug that was approved by the FDA in 2007. The route depicted delivered the API in 35% overall yield (nine steps).