A facile introduction of [14C]-carboxylic acid functionality, synthesis of carbon-14 labeled SB 209670 and SB 21742

被引:0
|
作者
Mokhallalati, MK [1 ]
Landvatter, SW [1 ]
Baine, NH [1 ]
机构
[1] SmithKline Beecham Pharmaceut, Chem R&D, Dept Synthet Chem, King Of Prussia, PA 19406 USA
来源
SYNTHESIS AND APPLICATIONS OF ISOTOPICALLY LABELLED COMPOUNDS 1997 | 1998年
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中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
An efficient method for the introduction of the C-14-carboxylic acid functionality was developed. This was accomplished by treating a methyl ester with LDA and then with isopropyl [carbonyl-C-14]chloroformate to form a mixed malonate. Selective decarboxylation of the methyl eater affored a carbon-14 labeled isopropyl ester. This method was used to prepare both of SE 209670-[C-14] and SE 217242-[C-14]. [GRAPHIC].
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页码:157 / 160
页数:4
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