2 H 5 ]-Amprenavir and [ 2 H 5 ]-saquinavir have been prepared from a common labeled precursor (1S, 2S)-(1-oxiranyl-2-[ 2 H 5 ]phenylethyl)-carbamic acid tert-butyl ester, 1. Both of these compounds are in the 'HEA' class of HIV protease inhibitors. [ 2 H 5 ]-Indinavir, a representative of the 'H
Isotope labeled ‘HEA Moiety’ in the synthesis of labeled HIV-protease inhibitors – Part 1
✍ Scribed by I. Victor Ekhato; Yuan Liao; Mihaela Plesescu
- Publisher
- John Wiley and Sons
- Year
- 2004
- Tongue
- French
- Weight
- 176 KB
- Volume
- 47
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.870
No coin nor oath required. For personal study only.
✦ Synopsis
Abstract
[(S)‐1′‐((N‐tert‐Butyloxycarbonyl)amino)‐2S‐[^2^H~5~]phenyl‐ethyl]oxirane 11, made from [^2^H~5~]‐bromobenzene, was transformed into the HIV‐protease inhibitors [^2^H~5~]‐DPH 153893 and [^2^H~5~]‐DPH 140662. Both compounds are members of the hydroxyethylamine class of protease inhibitors (HIV‐PIs). The method of synthesis is applicable to members of this class and the HEE group of HIV‐PIs. Copyright © 2004 John Wiley & Sons, Ltd.
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