Journal of labelled compounds and radiopharmaceuticals p. 179 - 193 (2005)
Update date:2022-07-29
Topics:
Ekhato, I. Victor
Liao, Yuan
Plesescu, Mihaela
[2H5]-Amprenavir and [2H 5]-saquinavir have been prepared from a common labeled precursor (1S, 2S)-(1-oxiranyl-2-[2H5]phenylethyl)-carbamic acid tert-butyl ester, 1. Both of these compounds are in the 'HEA' class of HIV protease inhibitors. [2H5]-Indinavir, a representative of the 'HEE' group of protease inhibitors, has also been synthesized. In the case of indinavir, 1S-(2,2-dimethyl-8, 8a-dihydro-3aH-indeno-[1,2-d]-oxazol-3R-yl)-2- oxiranylmethyl-3-[2H5]phenylpropan-1-one, 11, provided the [phenyl-2H5]-HEE core structure for synthesis of the desired labeled compound. Copyright
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