- IMIDAZOPYRIDINE COMPOUNDS AND USES THEREOF
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This invention generally relates to substituted imidazopyridine compounds, particularly substituted 4-(imidazo[1,2-a]pyridin-2-yl)benzamide compounds and salts thereof. This invention also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), processes for making such a compound, and intermediates used in such processes.
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Paragraph 212
(2014/08/19)
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- Halogen-lithium exchange between substituted dihalobenzenes and butyllithium: Application to the regioselective synthesis of functionalized bromobenzaldehydes
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Halogen-lithium interconversion reactions between unsymmetrically substituted mono- and bifunctional dihalobenzenes C6H 3XHal2 and C6H2XYHal2 (Hal=Br, I; X, Y=F, OR, CF3, CH(OMe)2) and butyllithium were investigated. The resultant organolithium intermediates were converted into the corresponding benzaldehydes in moderate to good yields. As a rule, bromine atoms in the position ortho to the functional group were replaced preferentially with lithium. Intramolecular competition experiments with bifunctional systems revealed that fluorine is capable of activating the neighboring bromine atom more strongly than methoxy and dimethoxymethyl groups. On the replacement of the non-activated bromine with iodine a complete reversal of this reactivity pattern can be accomplished due to the preferred iodine-lithium exchange.
- Da?browski, Marek,Kubicka, Joanna,Luliński, Sergiusz,Serwatowski, Janusz
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p. 6590 - 6595
(2007/10/03)
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