A modular approach to 4,5-diaminopyrrolo[2,3-d]pyrimidines and 2,4,5-triaminopyrrolo[2,3-d]pyrimidines |
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Authors: | Michael V. Voronkov Michael R. Becker |
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Affiliation: | Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, USA |
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Abstract: | A short and highly modular approach to various 4,5-diaminopyrrolo[2,3-d]pyrimidines and 2,4,5-triaminopyrrolo[2,3-d]pyrimidines was developed starting from 4-chloro-5-halopyrrolo[2,3-d]pyrimidines and 5-bromo-2,4-dichloropyrrolo[2,3-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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