58509-59-4Relevant articles and documents
CXCR2 ANTAGONIST
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Paragraph 0161-0163, (2020/11/23)
A compound as a CXCR2 antagonist and an application thereof in preparing a drug as a CXCR2 antagonist. In particular, the present invention relates to a compound represented by formula (II) or an isomer or pharmaceutically acceptable salt thereof.
Auxiliary-assisted palladium-catalyzed halogenation of unactivated C(sp3)-H bonds at room temperature
Yang, Xinglin,Sun, Yonghui,Sun, Tian-Yu,Rao, Yu
supporting information, p. 6423 - 6426 (2016/05/24)
The direct transformation of unactivated C(sp3)-H bonds into C-halogen bonds was achieved by palladium catalysis at room temperature with good functional group tolerance. Some drugs and natural products were readily modified by this method. Merged with substitution reaction, newly formed C-X bonds can be transformed into diverse C-O, C-S, C-C and C-N bonds. A preliminary mechanism study demonstrates that solvent is crucial for C-H activation and the C-H activation step is involved in the rate-limiting step. An isolated Pd(ii) intermediate can be transformed into a halogenated product with the retention of conformation which suggests that concerted reductive elimination from Pd(iv) to form a C-X bond was favored.
Room-temperature copper-catalyzed arylation of dimethylamine and methylamine in neat water
Wang, Deping,Kuang, Daizhi,Zhang, Fuxing,Yang, Chunlin,Zhu, Xiaoming
supporting information, p. 714 - 718 (2015/03/18)
The first room-temperature copper-catalyzed arylations of dimethylamine and methylamine in neat water have been developed. Using a combination of CuI and 6,7-dihydroquinolin-8(5 H)-one oxime as catalyst, dimethylamine is arylated with various aryl halides to give the corresponding products in good to excellent yields. Further, this catalysis enables the selective arylation of methylamine to afford the high yields of monoarylated methylamines as the sole products.
A highly efficient Cu-catalyst system for N-arylation of azoles in water
Wang, Deping,Zhang, Fuxing,Kuang, Daizhi,Yu, Jiangxi,Li, Junhua
supporting information; scheme or table, p. 1268 - 1271 (2012/06/04)
6,7-Dihydroquinolin-8(5H)-one oxime (L3) was found to serve as a superior ligand for the CuI-catalyzed N-arylation of imidazoles with aryl iodides, bromides, and electron-deficient chlorides in water. Moreover, the CuI/L3 catalyst system enabled the coupling reactions to take place smoothly with high yields under a low catalyst loading (0.1-1 mol% CuI and 0.2-2 mol% L3).
AMD070, a CXCR4 chemokine receptor antagonist: Practical large-scale laboratory synthesis
Crawford, Jason B.,Chen, Gang,Gauthier, David,Wilson, Trevor,Carpenter, Bryon,Baird, Ian R.,McEachern, Ernie,Kaller, Alan,Harwig, Curtis,Atsma, Bem,Skerlj, Renato T.,Bridger, Gary J.
, p. 823 - 830 (2013/01/03)
An efficient and convergent four-step synthetic route to the CXCR4 chemokine receptor antagonist AMD070 (1) has been developed which employs only a single chromatographic step in the entire sequence. Novel reductive amination methods have been developed for the coupling of 2 and 3 in which a dehydrative imine formation is followed by reduction with an attenuated borohydride reagent (zinc chloride and sodium borohydride). Selective extraction methods were employed to purify synthetic intermediates and remove reagents and impurities. A procedure has also been developed to isolate 1 in a pure crystalline form.
CYCLOALKANOPYRIDINE DERIVATIVE
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Page/Page column 86, (2010/11/24)
Provided are cycloalkanopyridine derivatives of formula [I]: [wherein the symbols are the same as those stated in the description]. The compounds act as a nociceptin receptor antagonist, and are useful as medicines for diseases associated with a nociceptin receptor, for example, as a reliever against tolerance to a narcotic analgesic; a reliever against dependence on or addiction to a narcotic analgesic; an analgesic enhancer; an antiobesitic or appetite suppressor; a treating or prophylactic agent for cognitive impairment and dementia/amnesia; an agent for treating developmental cognitive abnormality; a remedy for schizophrenia; an agent for treating neurodegenerative diseases; an anti-depressant or treating agent for affective disorder; a treating or prophylactic agent for diabetes insipidus; a treating or prophylactic agent for polyuria; or a remedy for hypotension.
Convenient synthesis of 5,6,7,8-tetrahydroquinolin-8-ylamine and 6,7-dihydro-5H-quinolin-8-one
McEachern,Yang,Chen,Skerlj,Bridger
, p. 3497 - 3502 (2007/10/03)
A novel two-step synthesis of 5,6,7,8-tetrahydroquinolin-8-ylamine, involving regioselective nitrosation of 5,6,7,8-tetrahydroquinoline followed by oxime reduction, is described. Oxime hydrolysis affords 6,7-dihydro-5H-quinolin-8-one.