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Synfacts 2010(12): 1340-1340  
DOI: 10.1055/s-0030-1258870
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of Tenofovir Disoproxil Fumarate

Contributor(s): Philip Kocienski
D. H. Brown Ripin*, D. S. Teager et al.*
Clinton Health Access Initiative, Boston, Howard University, Washington, Purdue University, West Lafayette and ProcesScience, Fayetteville, USA; University of Ottawa, Canada; Inogent Laboratories, Hyderabad and Aptuit Laurus Pvt., Hyderabad, India
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Publication History

Publication Date:
22 November 2010 (online)

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Significance

Tenofovir is a reverse transcriptase inhibitor used in combination with other antiretroviral agents for the treatment of HIV and chronic hepatitis B. It is administered once daily as the ­hydrolytically labile prodrug tenofovir disoproxil fumarate. The route depicted is a substantially optimized version of the manufacturing route that increased the overall yield from 13% to 24%.