On December 4, 2008, Geneste, Herve; Sauer, Daryl; Braje, Wilfried; Amberg, Wilhelm; Mezler, Mario; Bakker, Margaretha Henrica Maria published a patent.Related Products of 16296-68-7 The title of the patent was Preparation of heterocyclic compounds, in particular pyrazole derivatives as positive modulators of metabotropic glutamate receptor 2 (mGlu2 receptor). And the patent contained the following:
Title compounds I [X = O, S, S(O), S(O)2, NH, NHC(O), NRx or a chem. bond; Rx = (un)substituted alkyl, haloalkyl, cycloalkyl, alkoxy, haloalkoxy, Ph, 5- or 6-membered heteroaryl, etc.; Y = O, S, S(O), S(O)2, NH, NRx, (un)substituted O-phenylene, S-phenylene, NH-phenylene, or a chem. bond, A = alkylene; Ar = Ph or 5- or 6-membered heteroaryl; R1 = (un)substituted alkyl, alkoxy, haloalkyl, haloalkoxy, (un)substituted cycloalkyl, cycloalkyloxy, etc.; R2 = H, CN, OH, halo, (un)substituted alkyl, cycloalkyl, haloalkyl, alkoxy or haloalkoxy, or R1 and R2 may together with adjacent carbon atom which they bound form a (un)substituted 5- or 6-membered heterocyclic ring fused to the benzene ring; R3 = H, halo, (un)substituted alkyl, haloalkyl, alkoxy or haloalkoxy or (un)substituted cycloalkyl; Het = (un)substituted 5- or 6-membered (un)saturated or aromatic heterocycle], and their pharmaceutically acceptable salts or tautomers, are prepared and disclosed as pos. modulators of metabotropic glutamate receptor. Thus, e.g., II was prepared by reductive amination of 3-(thiophen-2-yl)-1H-pyrazole-4-carboxaldehyde with 1-(4-aminophenyl)butan-1-one. Selected compounds of the invention had activity in potentiating the mGlu2 receptor in the FLIPR assay, generally with an EC50 of < 10 μM, e.g., II showed EC50 value of < 1 μM as potentiator of mGlu2 receptor. The invention also relates to the use of these compounds for preparing a pharmaceutical composition and to a method of treating a medical disorder, selected from neurol. and psychiatric disorders associated with glutamate dysfunction. The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).Related Products of 16296-68-7
The Article related to pyrazole derivative preparation metabotropic glutamate mglu2 receptor modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 16296-68-7
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem