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Isotope labeled ‘HEA/HEE’ moiety in the synthesis of labeled HIV-protease inhibitors—Part II

✍ Scribed by I. Victor Ekhato; Yuan Liao; Mihaela Plesescu

Publisher
John Wiley and Sons
Year
2005
Tongue
French
Weight
220 KB
Volume
48
Category
Article
ISSN
0022-2135

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✦ Synopsis

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 'HEE' group of protease inhibitors, has also been synthesized. In the case of indinavir, 1S-( 2

phenylpropan-1-one, 11, provided the [phenyl-2 H 5 ]-HEE core structure for synthesis of the desired labeled compound.

📜 SIMILAR VOLUMES

Isotope labeled ‘HEA Moiety’ in the synt
Isotope labeled ‘HEA Moiety’ in the synthesis of labeled HIV-protease inhibitors – Part 1
✍ I. Victor Ekhato; Yuan Liao; Mihaela Plesescu 📂 Article 📅 2004 🏛 John Wiley and Sons 🌐 French ⚖ 176 KB

## 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 pr