AROMATIC FLUORINATIONS SUITABLE FOR F-18 LABELING OF ESTROGENS
AROMATIC FLUORINATIONS SUITABLE FOR F-18 LABELING OF ESTROGENS
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DOI：
10.1021/jo00325a017
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发表时间：
1981-01-01
影响因子：
3.6
通讯作者：
KILBOURN, MR
中科院分区：
文献类型：
--
作者：
NG, JS;KATZENELLENBOGEN, JA;KILBOURN, MR
研究了两种芳香族化合物的标记方法，芳基叠氮化合物的分解和芳基三氮烯的分解，作为潜在的适合于雌激素的氟-18标记的方法。芳基三氮烯方法在许多体系中得到中等的产率，但不能用于邻甲氧基或（甲磺酰基）氧基。芳基叠氮化物法得到了很好的对氟苯胺产率，它可以很容易地脱氨基，但氧或大的烷基邻位的叠氮化物干扰脱氨基。报道了芳基三氮烯分解法合成间氟己雌酚。
Two aromatic fluorination methods, the decomposition of aryl azides andthe decomposition of aryltriazenes, were investigated as methods potentially suitable for fluorine-18 labeling of estrogens. The aryltriazene method gives moderateyields in many systems but fails with o-methoxy or (methanesulfonyl) oxy groups. The aryl azide method gives good yields of p-fluoroanilines, which can be deaminated readily, but oxygen or large alkyl groups ortho to theazide interfere with the fluorination. The synthesis of m-fluorohexestrol via the aryltriazene decomposition approach is reported.