Journal of labelled compounds and radiopharmaceuticals p. 103 - 111 (2000)
Update date:2022-08-04
Topics:
Chen, Huixiong
Bischoff, Laurent
Fournie-Zaluski, Marie-Claude
Roques, Bernard P.
2(S)-benzyl-3-[hydroxy(1'(R)-aminoethyl)phosphinyl]propanoyl-L-3-[125I]-iodo tyrosine was prepared from 1(R)-(N-benzyloxycarbonylamino)ethylphosphinic acid in a six step synthesis. This new iodinated compound, which is a highly efficient aminopeptidase N inhibitor (Ki = 0.95 nM), can be used for complete characterization of the biochemical and pharmacological properties of aminopeptidase N and its in vivo inhibition. A high radiochemical purity was obtained with a specific activity of 2.17 Ci/mmol at the end of the synthesis.
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