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Synfacts 2019; 15(11): 1310
DOI: 10.1055/s-0039-1690282
DOI: 10.1055/s-0039-1690282
Chemistry in Medicine and Biology
Pre-Exposure Prophylaxis (PrEP)
Further Information
Publication History
Publication Date:
18 October 2019 (online)

Significance
Pre-exposure prophylaxis (PrEP) is a HIV prevention method for uninfected individuals. It virtually eliminates the risk of getting HIV if taken consistently and correctly. Truvada is the drug used for PrEP. It contains a combination of emtricitabine and tenofovir disoproxil fumarate (prodrug).
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Comment
Emtricitabine was synthesized by nucleosidation of a readily available oxathiolane derivate with the silylated nucleobase B. The high level of stereoselectivity is provided by in situ complexation of the oxathiolane and the Lewis acid. Tenofovir was synthesized in just six steps starting from commercially available (S)-glycidol.
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