Synthesis of 2(S)-benzyl-3-[hydroxy(1?(R)-amino ethyl)phosphinyl]propanoyl-L-3-[125I]-iodotyrosine: a radiolabelled inhibitor of aminopeptidase N
Résumé
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 217 Ci/mmol at the end of the synthesis. Copyright © 2000 John Wiley & Sons, Ltd.