- A new pathway to substituted 6-chloro-2-pyridinecarboxylic acid derivatives from the reaction of 4,6-dichloro-2-oxa-5-azabicyclo[2.2.2]oct-5-en-3-ones with nucleophiles
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Reaction of alcohols or amines with 4,6-dichloro-2-oxa-5-azabicyclo[2.2.2]oct-5-en-3-ones gives direct conversion into (3,(4,))5-substituted 6-chloro-2-pyridinecarboxylic acid derivatives via selective lactone cleavage followed by rapid elimination of HCl and H2O in the presence of DBU. Copyright
- Dubois, Kristof J.,Hoornaert, Georges J.
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- POSITIVE ALLOSTERIC MODULATORS OF MGLUR2
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The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved
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