- Process for the synthesis of oxazolopyridine compounds
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Process for the synthesis of compounds of formula (I): STR1 their pyridinium salts and N-oxides, in which formula: the nitrogen of the pyridine ring is situated in the α-, β-, γ- or δ-position with respect to the ring junction; R1 represents a halogen, a substituted or unsubstituted alkyl, a substituted or unsubstituted alkoxy or a nitro, substituted or unsubstituted amino, phenyl or cyano group; 0≤m≤2; R2 represents a lower alkyl or cycloalkyl group, a 5- or 6-membered heterocycle containing 1 or 2 hetero atoms, substituted or otherwise, or an aryl group STR2 such that: R3 represents a halogen, a substituted or unsubstituted alkyl, a substituted or unsubstituted alkoxy or a nitro, phenyl, substituted or unsubstituted sulfonyl, cyano, thioalkyl, substituted or unsubstituted amino, substituted or unsubstituted sulfinyl, mercapto, hydroxyl or ester group, 0≤n≤5 employing trimethylsilyl polyphosphate (PPSE) as a cyclization agent and enabling the compounds of formula (I) to be obtained in virtually quantitative yields. The compounds of formula I have anti-inflammatory, analgesic, and antipyretic activity.
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- A New Convenient Synthesis of 2-Aryl- and 2-Heteroaryloxazolopyridines
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Several 2-aryl- and 2-heteroaryloxazolopyridines were synthesized in high yields from 3-(arylcarbonylamino)-2-chloropyridines by heating in the presence of trimethylsilylpolyphosphate ester.
- Flouzant, Christine,Guillaumet, Gerald
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