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Updated: Aug 18, 2026

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 9, 2014
An efficient, scalable synthesis of the HIV reverse transcriptase inhibitor Ziagen (1592U89)
S M Daluge1, M T Martin, B R Sickles
1Division of Medicinal Chemistry, Glaxo Wellcome Inc., Research Triangle Park, North Carolina 27709, USA.
Abstract:
Ziagen, (1S,cis)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]- 2-cyclopentene-1-methanol, was synthesized from (1S,4R)-azabicyclo[2.2.1]hept-5-en-3-one by efficient processes which bypass problematic steps in earlier routes. 2-Amino-4,6-dichloro-5-formamidopyrimidine is a key intermediate which makes possible an efficient construction of the purine from a chiral cyclopentenyl precursor.
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