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Synthesis of a labeled inhibitor of HIV‐1 attachment: 1‐(4‐benzoylpiperazin‐1‐yl)‐2‐(4,7‐dimethoxy‐1H‐pyrrolo[2,3‐c]pyridinyl‐3‐yl‐[U‐ 14 C]ethane‐1,2‐dione, BMS‐488043‐ 14 C
Author(s) -
Ekhato I. Victor,
Rinehart J. Kent
Publication year - 2010
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1856
Subject(s) - chemistry , oxalyl chloride , acylation , yield (engineering) , human immunodeficiency virus (hiv) , friedel–crafts reaction , stereochemistry , chloride , medicinal chemistry , combinatorial chemistry , organic chemistry , virology , catalysis , materials science , metallurgy , biology
BMS‐488043 is a potent inhibitor of the interaction between HIV‐1 gp120 and the host cell receptor CD4. We prepared the carbon‐14‐labeled version to support preclinical studies of the compound. It was prepared from ethyl [U‐ 14 C]oxalyl chloride by a sequence using Friedel–Crafts acylation reaction. The overall radiochemical yield was 82% with a purity of >99.9%. Copyright © 2010 John Wiley & Sons, Ltd.