SYNTHESIS OF C-11 LABELED CALCIUM-CHANNEL ANTAGONISTS

被引：5

作者：

HOLSCHBACH, M

RODEN, W

HAMKENS, W

机构：

[1] Institute of Medicine Research Center, Jülich

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1991年 / 29卷 / 04期

关键词：

C-11-LABELED 1,4-DIHYDROPYRIDINES; SYNTHESIS; CALCIUM CHANNEL ANTAGONISTS;

D O I：

10.1002/jlcr.2580290408

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

A useful synthetic approach to carbon-11 labelled 1,4-dihydropyridines is described. Carbon-11 labelled calcium channel antagonists C-11-Nifedipine, C-11-Nisoldipine, C-11-Nitrendipine and C-11-CF3-Nifedipine were synthesized by a modified Hantzsch method using protected carboxy functions. Deprotection of the carboxylic acids by alkaline hydrolysis followed by conversion into the corresponding potassium salts and subsequent methylation with CH-11(3)I produced the labelled compounds in very good chemical and radiochemical yields (94%).

引用

页码：431 / 442

页数：12

共 20 条

[1] SYNTHESIS OF CARBOXY-NIFEDIPINE AND ITS USE IN THE PREPARATION OF AN AFFINITY RESIN FOR THE 1,4-DIHYDROPYRIDINE RECEPTOR [J].