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Synthesis of 6-acrylamido-4-(2-[18F]fluoroanilino)quinazoline: a prospective irreversible EGFR binding probe

โœ Scribed by Neil Vasdev; Peter N. Dorff; Andrew R. Gibbs; Erathodiyil Nandanan; Leanne M. Reid; James P. O'Neil; Henry F. VanBrocklin

Book ID
102375114
Publisher
John Wiley and Sons
Year
2005
Tongue
French
Weight
104 KB
Volume
48
Category
Article
ISSN
0022-2135

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โœฆ Synopsis

Acrylamido-quinazolines substituted at the 6-position bind irreversibly to the intracellular ATP binding domain of the epidermal growth factor receptor (EGFR). A general route was developed for preparing 6-substituted-4-anilinoquinazolines from [ 18 F]fluoroanilines for evaluation as EGFR targeting agents with PET. By a cyclization reaction, 2-[ 18 F]fluoroaniline was reacted with N 0 -(2-cyano-4-nitrophenyl)-N,N-dimethylimidoformamide to produce 6-nitro-4-(2-[ 18 F]fluoroanilino)quinazoline in 27.5% decay-corrected radiochemical yield. Acid mediated tin chloride reduction of the nitro group was achieved in 5 min (80% conversion) and subsequent acylation with acrylic acid gave 6-acrylamido-4-(2-[ 18 F]fluoroanilino)quinazoline in 8.5% decay-corrected radiochemical yield, from starting fluoride, in less than 2 h.

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