## 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
Synthesis of PNU-159548 labelled with 14C and 2H
✍ Scribed by C. Felicini; E. Fontana
- Publisher
- John Wiley and Sons
- Year
- 2002
- Tongue
- French
- Weight
- 99 KB
- Volume
- 45
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.580
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✦ Synopsis
Abstract
The cytotoxic antitumor compound PNU‐159548 (1) has been labelled with ^14^C and ^2^H. A three‐step sequence starting from [14‐^14^C]idarubicin (2a) led to radiochemically pure (>98%) [14‐^14^C]PNU‐159548 with a specific activity of 1.13 GBq/mmol. The synthesis of [^2^H~4~]PNU‐159548 was carried out in a similar manner starting from [1,1,2,2‐^2^H~4~]2‐bromoethanol (3b). Copyright © 2002 John Wiley & Sons, Ltd.
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## Abstract The arylpiperazine PNU‐243922 (**1**) has been labelled with ^14^C. A two‐step sequence starting from the ^14^C labelled alcohol **6a** led to radiochemically pure (>98%) [^14^C]PNU‐243922 with a specific activity of 546 MBq/mmol Copyright © 2002 John Wiley & Sons, Ltd.
A synthesis of dibucaine labeled with l"C in the heterocyclic ring is described. starting with isatin and acetic anh~dride-2-~"C as shown in Scheme I. Two deutero analogs, dibucaine-d2 and dibucaine-dg, were also synthesized by the reactions shown in Scheme 11. Dibucaine-dg was synthesized by conden
The preparation of deuterium labeled fexinidazole, a 5‐nitroimidazole drug candidate for the treatment of Human African Trypanosomiasis, and its two main metabolites (fexinidazole sulfoxide and fexinidazole sulfone) for use as internal standards for liquid chromatography‐mass spectrometry are report