- AMINO TRIAZOLES AS PI3K INHIBITORS
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The invention relates to compounds of formula (I) Said compounds are useful as protein kinase inhibitors, especially inhibitors of P13K, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.
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Page/Page column 47
(2009/07/03)
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- Unusual sterically controlled regioselective lithiation of 3-bromo-5-(4,4′-dimethyl)oxazolinylpyridine. Straightforward access to highly substituted nicotinic acid derivatives
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(Chemical Equation Presented) Lithiation of 5-bromonicotinic acid protected as secondary or tertiary amide as well as (4,4′-dimethyl)oxazoline with lithium amides is reported. The unusual C-2 and C-4 regioselective lithiation of 3-bromo-5-(4,4′-dimethyl)oxazolinylpyridine using LTMP versus LDA was observed, providing a new route to substituted nicotinic acid scaffolds. The methodology was applied to the synthesis of novel C-4 and C-6 arylated 5-bromonicotinic acids.
- Robert, Nicolas,Bonneau, Anne-Laure,Hoarau, Christophe,Marsais, Francis
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p. 6071 - 6074
(2007/10/03)
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