SYNTHESIS OF [2-C-14] FANTOFARONE OR 1-[4-[3-N-METHYL N-[3,4-DIMETHYL BETA-PHENETHYL] AMINO PROPYLOXY] BENZENE SULFONYL] 2-ISOPROPYL [2-C-14] INDOLIZINE

被引:1
|
作者
POINTEAU, P [1 ]
BERGER, Y [1 ]
机构
[1] SANOFI RECH,F-34184 MONTPELLIER 04,FRANCE
关键词
INDOLIZINE; C-14; CALCIUM ANTAGONIST;
D O I
10.1002/jlcr.2580341104
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Sodium [1-C-14] isobutyrate : 1 was obtained by carbonation of isopropyl magnesium bromide with (CO2)-C-14. From : 1 [1-C-14] isobutyryl chloride : a was prepared, which through the successive actions of diazomethane and hydrogen bromide gave rise to 1-bromo 3 methyl [2-C-14] 2-butanone: 5. The latter lead to the indolizine : 6 which by a route patterned after that used to make unlabelled Fantofarone gave the [2-C-14-indolizyl] Fantofarone : 8 (specific radioactivity : 58.2 mCi/mMole) overall yield 9.9% based on [C-14] BaCO3.
引用
收藏
页码:1023 / 1029
页数:7
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