A flexible synthesis of C-6 and N-1 analogues of a 4-amino-1,3-dihydroimidazo[4,5-c]pyridin-2-one core |
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| Authors: | Duncan A. Hay Fiona M. AdamGerwyn Bish Frederick CaloRachel Dixon M. Jonathan FrayJames Hitchin Peter JonesMichael Paradowski Gemma C. ParsonsKatie J.W. Proctor David C. PrydeNicholas N. Smith Thien-Duc Tran |
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| Affiliation: | a WorldWide Medicinal Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK
b SRG, London Office, 16 St. Helen′s Place, London EC3A 6DF, UK |
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| Abstract: | A flexible route which enables access to derivatives of 4-amino-1,3-dihydroimidazo[4,5-c]pyridin-2-ones is described. Issues of selectivity, reaction safety, and low yields in original routes are overcome with the key improvements to the route, including a Negishi cross-coupling and use of a carbamate as a protecting group and intrinsic carbonyl source. The new route enables variation of C-6 and N-1 substituents. |
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| Keywords: | TLR7 Negishi Carbamates Heterocycles |
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