FACILE PREPARATION OF (S)-N-[(1-ETHYL-2-PYRROLIDINYL)METHYL]-2,3-DIMETHOXY-5-(TRIBUTYLTIN)BENZAMIDE FROM ISOREMOXIPRIDE - THE PRECURSOR OF (I-125)EPIDEPRIDE AND (I-123)EPIDEPRIDE

被引:10
作者
DEPAULIS, T
SMITH, HE
机构
[1] Department of Chemistry, Vanderbilt University
关键词
D O I
10.1080/00397919108019800
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
[I-125]Epidepride, (S)-(-)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[I-125]iodo-2,3-dimethoxybenzamide ([I-125]NCQ 219), is a new, extremely potent radioligand, useful in the study of the distribution of the dopamine D-2 receptors in the brain. Its synthesis requires radioiodination of the corresponding 5-(tributyltin) derivative. The aryltin precursor (TDP 526) can be conveniently prepared in high yield from isoremoxipride (FLB 457) by tetrakis(triphenyl-phosphine)palladium(0)-catalyzed stannylation using bis(tri-n-butyltin) in triethylamine. An improved method for the preparation of isoremoxipride from o-vanillin was developed.
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页码:1091 / 1095
页数:5
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