## 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]Bros
Isotopic labeling of 2-desoxoparaherquamide A (PNU-141962) with deuterium
✍ Scribed by Byung H. Lee
- Publisher
- John Wiley and Sons
- Year
- 2002
- Tongue
- French
- Weight
- 113 KB
- Volume
- 45
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.624
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✦ Synopsis
Abstract
Modifications of marcfortine A and paraherquamide A led to the discovery of 2‐desoxoparaherquamide A (PNU‐141962, 3) which is as active as paraherquamide A and has an improved safety profile. In order to do preclinical studies, we wished to synthesize isotope‐labeled PNU‐141962. This account will describe the synthesis of [CD~3~]‐2‐desoxoparaherquamide A (4). The deuterium product was prepared in anticipation of using a similar synthesis for the preparation of the corresponding ^14^C‐ and ^3^H‐labeled products. Copyright © 2002 John Wiley & Sons, Ltd.
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## Abstract Alkaline treatment of nonsteroidal antiinflammatory 2‐arylpropionic acids in deuterium oxide led in all cases to isotopic exchange of the proton located at the α‐position of the side chain. Monodeuteration was observed in the case of carprofen, ibuprofen, ketoprofen, fenoprofen, flurbip