294181-97-8Relevant academic research and scientific papers
Manufacturing method of making heteroarylacetic compd. defluoromethyl
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Paragraph 0110-0112, (2018/10/03)
PROBLEM TO BE SOLVED: To provide a method for easily producing a difluoromethyl heteroaryl compound with high yield at low cost. SOLUTION: In the method for producing the difluoro methyl heteroaryl compound, a halogenated heteroaryl compound and a α-silyldifluoro acetate ester compound are reacted with each other in the presence of a metal halogenated compound. COPYRIGHT: (C)2012,JPOandINPIT
NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
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Page/Page column 73-74, (2014/09/29)
The present invention relates to compounds of the formula (I), the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof. In formula I the variables Het, A, X, Y, Z, R1, R2, R3, R4, R5 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
A new method for aromatic difluoromethylation: Copper-catalyzed cross-coupling and decarboxylation sequence from aryl iodides
Fujikawa, Kenichi,Fujioka, Yasutaka,Kobayashi, Akira,Amii, Hideki
supporting information; experimental part, p. 5560 - 5563 (2011/12/05)
A new methodology for aromatic difluoromethylation is described. Aryl iodides reacted with α-silyldifluoroacetates upon treatment with copper catalyst in DMSO or DME to give the corresponding aryldifluoroacetates in moderate to good yields. The subsequent hydrolysis of aryldifluoroacetates and KF-promoted decarboxylation afforded a variety of difluoromethyl aromatics.
New antifungal 1,2,4-triazoles with difluoro(heteroaryl)methyl moiety
Eto, Hiromichi,Kaneko, Yasushi,Sakamoto, Takao
, p. 982 - 990 (2007/10/03)
New 1,2,4-triazoles (1) having a difluoro(heteroaryl)methyl moiety were designed and synthesized via 1-aryl-2,2-difluoro-2- (heteroaryl)ethanones (2), which were prepared by two routes starting from the reaction of ethyl 2,2- difluoro(heteroaryl)acetate with phenyllithiums (Route A) and from the reaction of chlorodifluoro(heteroaryl)methane with benzaldehydes (Route B). The compounds 1 except for 1g show antifungal activities against yeasts and filamentous fungi in vitro, especially (+)-If have equal or superior activities compared to those of itraconazole.
