199327-69-0Relevant articles and documents
Preparation method of vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitor Cediranib
-
, (2018/06/15)
The invention discloses a preparation method of a vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitor Cediranib. The chemical name of the VEGF receptor tyrosine kinase inhibitor Cediranib is 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline, the chemical formula is C25H27FN4O3, and the structural formula is shown in the description. A preparation technology which adopts readily-available raw materials and is economical and environmentally friendly is adopted, a process method suitable for industrial production is found, the preparation process is novel, and the reaction process is simplified, so that the reaction yield is increased; the preparation method has important significance to the improvement on the economical and socialbenefits of the Cediranib.
Preparation methods for drug cediranib treating non-small cell lung cancer and kidney cancer and intermediate thereof
-
Paragraph 0018; 0019; 0022, (2018/06/15)
The invention discloses preparation methods for a drug cediranib treating non-small cell lung cancer and kidney cancer and an intermediate thereof. The chemical name of the drug cediranib treating non-small cell lung cancer and kidney cancer is 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline, and the structural formula thereof is as shown in the description.The preparation methods are simple, the cediranib intermediate and 5-hydroxy-4-fluoro-2-methylindole are synthesized to obtain cediranib through a condensation reaction, so that the atom is more economical, the reaction is more selective, and the operation is more controllable, the preparation method for the cediranib is more controllable, the product quality is improved, and the economic technology of active ingredients is advanced.
Substituted 2-arylbenzothiazoles as kinase inhibitors: Hit-to-lead optimization
Tasler, Stefan,Mueller, Oliver,Wieber, Tanja,Herz, Thomas,Pegoraro, Stefano,Saeb, Wael,Lang, Martin,Krauss, Rolf,Totzke, Frank,Zirrgiebel, Ute,Ehlert, Jan E.,Kubbutat, Michael H.G.,Schaechtele, Christoph
supporting information; experimental part, p. 6728 - 6737 (2009/12/09)
Based on an (aminoaryl)benzothiazole quinazoline hit structure for kinase inhibition, a systematic optimization program resulted in a lead structure allowing for inhibitory activities in cellular phosphorylation assays in the low nanomolar range.
