On September 9, 2011, Layton, Mark E.; Kelly, Michael J.; Hartingh, Timothy J. published a patent.Application In Synthesis of [4-Fluoro-3-(tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]methanol The title of the patent was Preparation of benzothiadiazole and thiadiazolopyridine dioxides as positive allosteric modulators of mGluR2. And the patent contained the following:
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 neurol. and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The compounds of the invention have general formula I, wherein X is C or N; Y is C1-6 alkyl; R1 is (un)substituted benzyl, (un)substituted C2-8 alkyl, etc.; each R2 is independently halo, OH, C1-4 alkyl, etc.; A is (un)substituted aryl or (un)substituted heteroaryl. 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. Synthetic procedures for preparing I are exemplified. Example compound II, prepared in a 5-step synthesis that culminated in reaction of III with 2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile, potentiated mGluR2 activity in a FLIPR assay with an EC50 of 5.0 nM. The experimental process involved the reaction of [4-Fluoro-3-(tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]methanol(cas: 1333264-06-4).Application In Synthesis of [4-Fluoro-3-(tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]methanol
The Article related to benzothiadiazole thiadiazolopyridine dioxide preparation allosteric mglur2 modulator therapy, neurol psychiatric disorder treatment benzothiadiazole thiadiazolopyridine dioxide and other aspects.Application In Synthesis of [4-Fluoro-3-(tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]methanol
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