Synthesis of aryl [35S]sulfones:: Friedel-Crafts sulfonylation of aryl ethers with high specific activity [35S]methanesulfonyl chloridet

被引:7
|
作者
Wallace, Michael A. [1 ]
Raab, Conrad [1 ]
Dean, Dennis [1 ]
Melillo, David [1 ]
机构
[1] Merck Res Labs, Dept Drug Metab, Rahway, NJ 07065 USA
来源
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2007年 / 50卷 / 5-6期
关键词
S-35]methanesulfonyl chloride; aryl [S-35] sulfones; S-35] sulfone triflate;
D O I
10.1002/jlcr.1300
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Lewis acid-assisted sulforlylation of anisole with [S-35] methanesulfonyl chloride afforded high specific activity aryl [S-35] sulfones. Demethylation and treatment with triflic anhydride gave the versatile [S-35]triflate 1 in good overall yields. The [S-35] sulfone triflate could be further functionalized by catalyzed aminations, Stille couplings, and cyanation. Copyright (c) 2007 John Wiley & Sons, Ltd.
引用
收藏
页码:347 / 349
页数:3
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