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Rapid mild syntheses of [ 11 C]benzophenones by Pd(0)‐catalysed 11 C‐carbonylative coupling of iodoarenes with phenyltributylstannane in DME‐water
Author(s) -
AlQahtani Mohammed H.,
Pike Victor W.
Publication year - 2000
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 - 10.1002/1099-1344(200007)43:8<825::aid-jlcr367>3.0.co;2-a
Subject(s) - chemistry , carbon monoxide , palladium , carbonylation , dimethoxyethane , medicinal chemistry , radiochemistry , organic chemistry , catalysis , electrode , electrolyte
Palladium(0)‐catalysed 11 C‐carbonylative coupling of iodoarenes (RC 6 H 4 I; R=H, 2‐Me, 3‐Me, 4‐F, and 4‐CF 3 ) with phenyltributylstannane for 1 min in 1,2‐dimethoxyethane‐water (4: 1 v/v) at room temperature gave [ 11 C]benzophenones (RC 6 H 4 11 COPh) in high radiochemical yields (58–82%, decay‐corrected from trapped [ 11 C]carbon monoxide). The efficiency of [ 11 C]carbon monoxide trapping from a single pass into the reaction medium was 4·5–6·2%. The reaction conditions are suitable for the rapid, efficient introduction of cyclotron‐produced carbon‐11 ( t 1/2 =20·3 min) into substituted benzophenones as prospective labelling agents and radiopharmaceuticals for application in medical imaging with positron emission tomography. Copyright © 2000 John Wiley & Sons, Ltd.