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

页码：899 / 909

页数：11

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