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A modular approach to 4,5-diaminopyrrolo[2,3-d]pyrimidines and 2,4,5-triaminopyrrolo[2,3-d]pyrimidines
Authors:Michael V Voronkov  Michael R Becker
Institution:Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, USA
Abstract:A short and highly modular approach to various 4,5-diaminopyrrolo2,3-d]pyrimidines and 2,4,5-triaminopyrrolo2,3-d]pyrimidines was developed starting from 4-chloro-5-halopyrrolo2,3-d]pyrimidines and 5-bromo-2,4-dichloropyrrolo2,3-d]pyrimidine, respectively. Direct amination at the 5-position was achieved without the use of transition metals or other catalysts in 32-86% yield. Ten examples are given.
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