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Labelled compounds of interest as antitumour agents – VIII. Synthesis of 2H-isotopomers of pentamethylmelamine and of a potential prodrug thereof

✍ Scribed by Sandra Ferrer; Declan P. Naughton; Michael D. Threadgill

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

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✦ Synopsis

Abstract

Treatment of 2‐chloro‐4,6‐(dimethylamino)‐1,3,5‐triazine with trideuteromethylamine gave 4,6‐(dimethylamino)‐2‐trideuteromethyl‐1,3,5‐triazine, an isotopomer of the experimental anticancer agent pentamethylmelamine (PMM). Mitsunobu coupling with 1,2‐dimethyl‐3‐hydroxymethyl‐5‐methoxy‐indole‐4,7‐dione gave 1,2‐dimethyl‐3‐(N‐(4,6‐bis(dimethylamino)‐1,3,5‐triazin‐2‐yl)‐N‐trideuteromethylaminomethyl)‐5‐methoxyindole‐4,7‐dione. This conjugate is a potential reductively triggered prodrug of PMM. Copyright © 2002 John Wiley & Sons, Ltd.

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