1139901-87-3Relevant articles and documents
Nickel-catalyzed biaryl coupling of heteroarenes and aryl halides/triflates
Canivet, Jerome,Yamaguchi, Junichiro,Ban, Ikuya,Itami, Kenichiro
, p. 1733 - 1736 (2009)
Ni-based catalytic systems for the arylation of heteroarenes with aryl halides and triflates have been established. Ni(OAc)2/bipy is a general catalyst for aryl bromides/iodides, and Ni(OAc)2/dppf is effective for aryl chlorides/triflates. Thiazole, benzothiazole, oxazole, benzoxazole, and benzimidazole are applicable as heteroarene coupling partners. A rapid synthesis of febuxostat, a drug for gout and hyperuricemia, is also demonstrated.
Synthesis and bioevaluation of 1-phenyl-pyrazole-4-carboxylic acid derivatives as potent xanthine oxidoreductase inhibitors
Li, Jing,Wu, Fangping,Liu, Xingguo,Zou, Yake,Chen, Huixiong,Li, Zheng,Zhang, Lei
, p. 20 - 30 (2017/09/19)
A diverse library of 1-phenyl-pyrazole-4-carboxylic acid derivatives were synthesized and evaluated for their inhibitory potency against xanthine oxidoreductase (XOR) in vitro and vivo, and the structure-activity relationship (SAR) analyses were also pres
A 2- aryl residue nitrile method for the preparation of thiazole derivatives
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Paragraph 0083; 0084, (2017/03/21)
The invention discloses a novel intermediate (II) and a method for preparing a 2-arylnitrile-thiazole derivative (I) by a coupling reaction of the novel intermediate (II) and a compound shown in the formula (III). In the formulas, X represents Cl, Br or I, Y represents F, Cl, Br, I, N2, -OSO2Ra, -OCORa or -OSi(Ra)3, R1 represents C1-6 alkyl or C6-10 aryl, Ra represents C1-6 alkyl or C6-10 aryl, and the C1-6 alkyl or C6-10 aryl is independently and optionally replaced. The preparation method has the advantages of mild technical conditions, less impurities, simple processes, safety and controllability and low energy consumption and is especially suitable for industrial production. The invention also discloses a method for preparing the novel intermediate shown in the formula (II). The preparation method utilizes cheap materials, is free of separation purification and greatly reduces a reaction cost.
Facile one-pot transformation of arenes into aromatic nitriles under metal-cyanide-free conditions
Tamura, Toshiyuki,Moriyama, Katsuhiko,Togo, Hideo
, p. 2023 - 2029 (2015/03/18)
Electron-rich arenes bearing methyl or methoxy groups on the aromatic ring were treated with dichloromethyl methyl ether and ZnBr2, and then with molecular iodine and aq. ammonia to give the corresponding aromatic nitriles in good yields. Using this method, febuxostat was efficiently prepared from 4-bromophenol in four steps. The method can be used for the preparation of aromatic nitriles from arenes in one pot under metal-cyanide-free conditions. Various electron-rich arenes could be effectively converted into the corresponding aromatic nitriles in good yields, by treatment with ZnBr2 and dichloromethyl methyl ether, followed by reaction with molecular iodine and aq. ammonia.
PROCESS FOR PRODUCING PHENYL-SUBSTITUTED HETEROCYCLIC DERIVATIVE THROUGH COUPLING USING TRANSITION METAL CATALYST
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Page/Page column 17, (2012/01/13)
A process for efficiently producing, through few steps either a xanthine oxidase inhibitor, which is a therapeutic agent for hyperuricemia, or an intermediate therefore. The process is a novel coupling process which comprises subjecting a compound represented by formula (1) to coupling reaction with a compound represented by formula (2) in the presence of a transition metal compound to thereby obtain a compound represented by formula (3).
