Synthesis of 1‐[4‐(m‐tolyl)amino‐6‐quinazolinyl]‐3‐[ 14 C]‐methyl triazene: a radiolabeled probe for the combi‐targeting concept | Zendy

Matheson Stephanie L. | Zendy; Mzengeza Shadreck | Zendy; JeanClaude Bertrand J. | Zendy

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Synthesis of 1‐[4‐(m‐tolyl)amino‐6‐quinazolinyl]‐3‐[ 14 C]‐methyl triazene: a radiolabeled probe for the combi‐targeting concept

Author(s) -

Matheson Stephanie L.,

Mzengeza Shadreck,

JeanClaude Bertrand J.

Publication year - 2003

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.713

Subject(s) - triazene , chemistry , alkylation , hydrolysis , liquid scintillation counting , quinazoline , stereochemistry , nuclear chemistry , radiochemistry , biochemistry , organic chemistry , catalysis

The synthesis of 1‐[4‐( m ‐tolyl)amino‐6‐quinazolinyl]‐3‐[ 14 C]‐methyl triazene (SMA41) is described. This triazene was designed to be hydrolyzed under physiological conditions to N 4 ‐ m ‐tolyl‐quinazoline‐4,6‐diamine (SMA52), a moderate inhibitor of the epidermal growth factor receptor (EGFR) and the DNA alkylating species [ 14 C]‐methyldiazonium. A radiolabeled probe was needed to test the hypothesis that in situ hydrolysis of SMA41 may induce alkylation of the ATP binding site of EGFR. 14 C‐SMA41 was obtained with a radiochemical yield of 21% and a specific activity of 54.6 mCi/mmol, as determined by HPLC quantitation and scintillation counting. Radio‐TLC analyses showed 98% radiochemical purity. Copyright © 2003 John Wiley & Sons, Ltd.

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