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Synthesis of Brostallicin (PNU-166196A) Labelled with 2H and 14C

✍ Scribed by E. Fontana; A. Pignatti

Publisher
John Wiley and Sons
Year
2002
Tongue
French
Weight
126 KB
Volume
45
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Brostallicin (PNU‐166196A), a DNA minor groove binder, has been labelled with ^2^H and ^14^C. The preparation of the deuterium specifically labelled [^2^H~4~]brostallicin was achieved according to a nine‐step sequence starting from 1,2‐diamino[1,1,2,2‐^2^H~4~]ethane (1). [^14^C]Brostallicin was obtained via a four‐step procedure in 31% overall radiochemical yield starting from 1‐methyl‐4‐nitropyrrole‐2‐[^14^C]carboxylic acid (9). Copyright © 2002 John Wiley & Sons, Ltd.

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