- Cross-coupling reaction of 2-halo1-methyl-1H-imidazo[4,5-b]pyridine offers a new synthetic route to mutagenic heterocyclic amine-PHIP and DMIP
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A modified synthetic approach to the synthesis of heterocyclic food mutagens, 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PHIP) and 2-amino-1,6-dimethylimidazo[4,5-b]pyridine (DMIP) is reported. This route highlights an optimized palladium catalysed Buchwald cross-coupling of 2-halo-1-methyl-imidazo[4,5-b]pyridine with benzophenoneimine followed by acidic hydrolysis to yield compound 7. Using finely tailored conditions, Suzuki cross-coupling reactions with highly efficient catalytic systems were performed as the final step on 8 to introduce the aryl group and methyl group on the heterocyclic core.
- Sajith, Ayyiliath M.,Muralidharan, Arayambath,Karuvalam, Ranjith P.,Haridas, Karickal R.
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p. 361 - 364
(2013/07/26)
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- TRIAZOLES AND THEIR USE AS BRADYKININ B1 RECEPTOR ANTAGONISTS
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Compounds of Formula (I): are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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Page/Page column 81
(2008/06/13)
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- Synthesis and Spectral Data of Pyrido-as-triazines
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The pyrido-as-triazine and its 3-phenyl derivatives were prepared via cyclisation with polyphosphoric acid of suitable 3-substituted 2-aminopyridines obtained by reduction of the corresponding 2-nitropyridines.The 3-substituted 2-nitropyridines wer
- Ple, N.,Queguiner, G.
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p. 475 - 476
(2007/10/02)
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