314267-83-9Relevant articles and documents
Preparation method of isoxazole derivative
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Paragraph 0090-0095, (2019/12/02)
The invention relates to a preparation method of an isoxazole derivative, which comprises the following steps of mixing an propargyl alcohol derivative, a halogen source, an acid and a solvent, and heating to react; adding the hydroxylamine into the react
Scalable synthesis of the VEGF-R2 kinase inhibitor JNJ-17029259 using ultrasound-mediated addition of MeLi-CeCl3 to a nitrile
Reuman, Michael,Beish, Sandra,Davis, Jeremy,Batchelor, Mark J.,Hutchings, Martin C.,Moffat, David F. C.,Connolly, Peter J.,Russell, Ronald K.
, p. 1121 - 1123 (2008/09/18)
(Chemical Equation Presented) The preparation of the selective VEGF-R2 kinase inhibitor 10 (JNJ-17029259) is described in which the key precursor, 4-(5-isoxazolyl)benzonitrile, undergoes clean transformation to the corresponding cumylamine derivative with
4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: Synthesis and biological evaluation
Hughes, Terry V.,Emanuel, Stuart L.,Beck, Amanda K.,Wetter, Steven K.,Connolly, Peter J.,Karnachi, Prabha,Reuman, Michael,Seraj, Jabed,Fuentes-Pesquera, Angel R.,Gruninger, Robert H.,Middleton, Steven A.,Lin, Ronghui,Davis, Jeremy M.,Moffat, David F.C.
, p. 3266 - 3270 (2008/02/09)
A novel series of 4-aryl-5-cyano-2-aminopyrimidines were synthesized and found to have potent VEGF-R2 kinase inhibitory activity. Structure-activity relationships were investigated and compound 14a was shown to be efficacious in a mouse model of corneal neovascularization.
