PREPARATION OF 1,2-DIMETHOXY-4-(BIS-DIETHYLAMINOETHYL-[C-14]-AMINO)-5-BROMOBENZENE

被引：0

作者：

WANG, TST ^{[1
]}

FAWWAZ, RA ^{[1
]}

VANHEERTUM, RH ^{[1
]}

机构：

[1] COLUMBIA UNIV COLL PHYS & SURG,DEPT RADIOL,DIV NUCL MED,NEW YORK,NY 10032

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1993年 / 33卷 / 11期

关键词：

ANTIMALARIAL AGENT; RC-12-[C-14; CHLORINATION; GRIGNARD REAGENT; BIS-N-ALKYLATION;

D O I：

10.1002/jlcr.2580331103

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

1,2-Dimethoxy-4-(bis-diethylaminoethyl-[C-14] -amino)-5-bromobenzene (III) was synthesized for in vivo pharmacokinetic and pharmacodynamic evaluation. The synthesis of (III) was easily obtained by the direct alkylation of 1,2-dimethoxy-5-bromo-aniline with beta-diethylaminoethyl chloride-ethylene-[C-14], using CH3MgCl as the proton abstractor. Compound III was obtained with a 22.3% yield. The specific activity was 2.2mCi/mmol, with a radiochemical purity of >99%.

引用

页码：1007 / 1012

页数：6