85148-26-1Relevant academic research and scientific papers
Preparation method of 2-chloro-3-trifluoromethylpyridine
-
Paragraph 0029-0061, (2021/01/25)
The invention discloses a preparation method of 2-chlorine- 3-trifluoromethylpyridine. The method comprises the following steps: (1), sequentially adding 2, 3, 6-trichloro-5-trifluoromethylpyridine, an acid-binding agent and a catalyst into a lower aliphatic alcohol solvent, and starting a circulating water pump to replace hydrogen in vacuum, with the addition amount of the catalyst being 0.01-0.5% of the reaction system; (2), controlling the temperature of the reductive dechlorination reaction to be -10-65 DEG C, the reaction hydrogen pressure to be 0.1-2.0 MPa and the reaction time to be 4-24 hours; and (3), filtering, rectifying and purifying the obtained reaction liquid in sequence to finish separation of corresponding products and unreacted raw materials. The preparation method of the2-chlorine-3-trifluoromethylpyridine, provided by the invention is simple in process, easy to operate and beneficial to industrial production, the obtained product is high in purity, the purity is greater than 98%, a plurality of useful products are produced at one time, and on the basis of the selectivity of the useful products, the selectivity is 95%, the conversion rate of a single raw material is over 95%, and the production cost is low.
Preparation method of chlorotrifluoromethylpyridine
-
Page/Page column 7-10, (2020/01/12)
The invention discloses a preparation method of chlorotrifluoromethylpyridine. The chlorotrifluoromethylpyridine is obtained by reacting 3-trifluoromethylpyridine with a chlorination reagent. The preparation method has the advantages of high selectivity and high yield of the product, mild process conditions and the like.
Efficient indium-mediated dehalogenation of aromatics in ionic liquid media
Canete, Alvaro F.,Salas, Cristian O.,Zacconi, Flavia C.
, p. 398 - 407 (2013/03/13)
An efficient indium-mediated dehalogenation reaction of haloaromatics and haloheteroaromatics in ionic liquids has been studied. This method is simple and effective in the presence of [bmim]Br. Furthermore, this methodology is environmentally friendly compared with conventional ones.
N-Phenyl-N′-[4-(5H-pyrrolo[3,2-d]pyrimidin-4-yloxy)phenyl]ureas as novel inhibitors of VEGFR and FGFR kinases
Oguro, Yuya,Miyamoto, Naoki,Takagi, Terufumi,Okada, Kengo,Awazu, Yoshiko,Miki, Hiroshi,Hori, Akira,Kamiyama, Keiji,Imamura, Shinichi
experimental part, p. 7150 - 7163 (2010/11/20)
We have recently reported the discovery of pyrrolo[3,2-d]pyrimidine derivatives 1a and 1b as potent triple inhibitors of vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), and Tie-2 kinases. To identify compounds having strong inhibitory activity against fibroblast growth factor receptor (FGFR) kinase, further modification was conducted using the co-crystal structure analysis of VEGFR2 and 1b. Among the compounds synthesized, urea derivative 11l having a piperazine moiety on the terminal benzene ring showed strong inhibitory activity against FGFR1 kinase as well as VEGFR2 kinase. A binding model of 11l complexed with VEGFR2 suggested that the piperazine moiety forms additional interactions with Ile1025 and His1026.
PYRIDYL DERIVATIVES AND THEIR USE AS MGLU5 RECEPTOR ANTAGONISTS
-
Page/Page column 28, (2008/06/13)
The present invention is directed toward pyridyl derivatives of formula (I) as antagonists of the mGlu5 receptor. As such the compounds may be useful for treatment or prevention of disorders remedied by antagonism of the mGlu5 receptor, wherein Ar is phenyl or napthyl each of which may be substituted by one or more C1-C4 alkyl, C1-C4 alkoxy, C1-C5 acyl, halo, amino, nitro, cyano, hydroxy, C1-C5 acylamino, C1-C4 alkylsulfonylamino, mono-, di- or trifluorinated C1-C3 alkyl, substituents which may be the same or different and may bear a CONH2, CONHCH3, CON(CH3)2, CO2H, CO2CH3, OCF3, CH2NHCOCH3, CH2NH2, CH2N(CH3)2, CH2CN, CH2OH, CH2NHSO2CH3, CH2N(CH3)(CH2)2 CN, CH2N(CH3)CH(CH3)2, CH2NHCH(CH3)2, CH2NH(CH2)2CH3, CH2NHCO2R4, CH2NHCH2CH3, CH2NHCH3 NHCOC(CH3)2, or N(S(O)2CH3)2 substituent; R1 is hydrogen, halo, R4, CN, C(NOH)R3, C(NO-R4)R3, (CH)2CO2R4 , (CH2)n OR3 , COR3 , CF3,SR4 , S(O)R4, S(O)2R4, COCH2CO2R3 , NHSO2R4 , NHCOR3, C(NOR3)NH2, CH2OCOR3,(CH2)n NH2, CON(CH3)2 (CH2)nNHCO2R4 , CO2R3, CONH2, CSNH2, C(NH)NHOR3, (CH2)nN(CH3)2, or CONHNHCOR3; R2 is 1,2-ethenediyl or 1,2-ethynediyl; R3 is hydrogen or C1-C4 alkyl; R4 is C1-C4 alkyl; and n is 0, 1, 2,3 or 4; or a pharmaceutically acceptable salt thereof, or an N-oxide thereof.
