Palladium(II)-mediated 11C-carbonylative coupling of diaryliodonium salts with organostannanes -: a new, mild and rapid synthesis of aryl [11C]ketones
Palladium(II)-mediated 11C-carbonylative coupling of diaryliodonium salts with organostannanes -: a new, mild and rapid synthesis of aryl [11C]ketones
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DOI：
10.1039/a907803g
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发表时间：
2000-01-01
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影响因子：
--
通讯作者：
Pike, VW
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文献类型：
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作者：
Al-Qahtani, MH;Pike, VW
钯(II)催化的二芳基碘盐与芳基三丁基锡在二甲醚-水(4：1v/v)中反应1min，可温和、快速地合成芳基[C-11]酮。取代的芳基三丁基锡与二苯基溴化碘偶联得到取代的[C-11]二苯甲酮，放化产率通常很高(>；98%，衰变校正后)，而在一个环中含有一个或两个取代基的二苯基碘对甲苯磺酸盐与苯基三丁基锡偶合得到取代的(30-43%)和未取代的[C-11]二苯甲酮(47-66%)的混合物。这些反应是将回旋加速器产生的碳-11(t(1/2)=20.4min)引入到潜在的放射性示踪剂中，用于正电子发射断层扫描的医学成像。
Palladium(II)-mediated [C-11]carbonylative coupling of diaryliodonium salts with aryltributylstannanes for 1 min in DME-water (4:1 v/v) at RT gives a new mild and rapid route to aryl [C-11]ketones. Substituted aryltributylstannanes couple with diphenyliodonium bromide to give substituted [C-11]benzophenones in generally very high radiochemical yield (> 98%, decay-corrected), while diphenyliodonium tosylates, bearing one or two substituents in one ring, couple with phenyltributylstannane to give a mixture of substituted (30-43%) and unsubstituted [C-11]benzophenone (47-66%). These reactions are highly attractive for introducing cyclotron-produced carbon-11 (t(1/2)=20.4 min) into prospective radiotracers for application in medical imaging with positron emission tomography.