Synthesis of brostallicin (PNU-166196A) labelled with 2H and 14C

被引：4
|
作者：
Fontana, E [1 ]
Pignatti, A [1 ]
机构：
[1] Pharmacia, Global Drug Metab Dept, I-20014 Nerviano, MI, Italy
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2002年 / 45卷 / 11期
关键词：
brostallicin; PNU-166196A; distamycin; minor groove binder; deuterium; Carbon-14;
D O I：
10.1002/jlcr.611
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
Brostallicin (PNU-166196A), a DNA minor groove binder, has been labelled with H-2 and C-14. The preparation of the deuterium specifically labelled [H-2(4)]brostallicin was achieved according to a nine-step sequence starting from 1,2-diamino[1,1,2.2-(2) H-4]ethane (1). [C-14]Brostallicin was obtained via a four-step procedure in 31% overall radiochemical yield starting from 1-methyl-4-nitropyrrole-2[C-14]carboxylic acid (9). Copyright (C) 2002 John Wiley Sons, Ltd.
引用
收藏
页码：899 / 909
页数：11
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