Isotope labeled 'HEA Moiety' in the synthesis of labeled HIV-protease inhibitors - Part 1

[(S)‐1′‐((N‐tert‐Butyloxycarbonyl)amino)‐2S‐[2H5]phenyl‐ethyl]oxirane 11, made from [2H5]‐bromobenzene, was transformed into the HIV‐protease inhibitors [2H5]‐DPH 153893 and [2H5]‐DPH 140662. Both compounds are members of the hydroxyethylamine class of protease inhibitors (HIV‐PIs). The method of sy...

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Bibliographic Details
Published in:Journal of labelled compounds & radiopharmaceuticals 2004-10, Vol.47 (12), p.821-835
Main Authors: Ekhato, I. Victor, Liao, Yuan, Plesescu, Mihaela
Format: Article
Language:English
Subjects:
[2H5]-HEA isostere
AIDS
anti-HIV
Biological and medical sciences
Contrast media. Radiopharmaceuticals
Medical sciences
Pharmacology. Drug treatments
protease inhibitor
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Summary:[(S)‐1′‐((N‐tert‐Butyloxycarbonyl)amino)‐2S‐[2H5]phenyl‐ethyl]oxirane 11, made from [2H5]‐bromobenzene, was transformed into the HIV‐protease inhibitors [2H5]‐DPH 153893 and [2H5]‐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.
ISSN:0362-4803
1099-1344
DOI:10.1002/jlcr.870