THE SYNTHESIS OF THE CARBONYL-C-14 ANALOG OF ZATOSETRON MALEATE, A POTENT, LONG-ACTING, ORALLY EFFECTIVE 5-HT3 RECEPTOR ANTAGONIST

被引：2

作者：

OBANNON, DD ^{[1
]}

WHEELER, WJ ^{[1
]}

机构：

[1] ELI LILLY & CO,LILLY RES LAB,LILLY CORP CTR,INDIANAPOLIS,IN 46285

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1991年 / 29卷 / 06期

关键词：

ZATOSETRON MALEATE; 5-HT3 RECEPTOR ANTAGONIST; C-14; LABELED;

D O I：

10.1002/jlcr.2580290603

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Endo-5-chloro-2,3-dihydro-2,2-dimethyl-N-(8-methyl-8-azabicyclo-[3.2.1.]-oct-3-yl-7-benzofurancarboxamide-[carbonyl-C-14] (Z)-2-butenedioate (zatosetron-[C-14] maleate,1), has been prepared from 5-chloro-7-bromo-2,3-dihydro-2,2-dimethylbenzofuran (5) in four radiochemical steps with the reaction of 5 with K14CN/CuCN as the key step. The synthesis of 5 from 2-bromo-4-chlorophenol is also outlined.

引用

页码：625 / 631

页数：7