Premium
Labelled compounds of interest as antitumour agents. Part III (1). Synthesis of 2 H and 3 H isotopomers of etanidazole (SR 2508)
Author(s) -
Webb Paul,
Threadgill Michael D.
Publication year - 1990
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.2580280304
Subject(s) - chemistry , isotopomers , acetamide , deuterium , sodium borohydride , kinetic isotope effect , aldehyde , radiochemistry , stereochemistry , organic chemistry , catalysis , physics , quantum mechanics , molecule
Chemically and radiochemically efficient syntheses of N‐(2‐hydroxy‐2‐[ 2 H]ethyl)‐2‐(2‐nitroimidazol‐l‐yl)acetamide and N‐(2‐hydroxy‐2‐[ 3 H]ethyl)‐2‐(2‐nitroimidazol‐1‐yl)acetamide, isotopomers of the hypoxic cell radiosensitiser etanidazole (SR 2508), have been achieved by reduction of the corresponding aldehyde with isotopically labelled sodium borohydride. The primary kinetic deuterium isotope effect for the process is 1.5.