199327-69-0Relevant articles and documents
Preparation methods for drug cediranib treating non-small cell lung cancer and kidney cancer and intermediate thereof
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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.
Preparation method of cediranib intermediate
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, (2018/07/06)
The invention discloses a preparation method of a cediranib intermediate. The cediranib intermediate has a chemical name as 4-chlorine-6-methoxy-7-[3-(pyrrolidine-1-base) propoxy] quinazoline, and hasa structural formula as shown in the below figure. According to the preparation method of the cediranib intermediate provided by the invention, 6-methoxy-7-hydroxy-3,4-dihydro quinazoline-4-ketone isadopted as a raw material, and condensation reaction, reduction reaction, cyclization reaction and chlorination reaction are carried out for preparing the cediranib intermediate, and the preparationmethod of the cediranib intermediate has no need to carry out group protection and deprotection for multiple times, and is mild in reaction conditions, low in cost, short in synthesis steps, less in byproduct, higher in total yield, and more suitable for industrial production.
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.