The Synthesis And Research Of The Derivates Of SU11248

SU11248, a multi-targeted receptor tyrosine kinase inhibitor of vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF)-receptors, In preclinicaltrial,this drug is effective for the GIST and MRCCThe target of the project is the synthesis of the derivatives of SU11248, mainly modifying the pyrrol ring . After gropeing, we have got two routes,the first one is that we got the pyrrol ring with t-butyl acetoacetate and acetoacetate in the classical knorr reaction ,and removing the Boc,through the vilsmeyer and hydrolyzation reaction;the second one is that we got the the pyrrol ring through the Knorr reaction, through the vilsmeyer and then replacing,and hydrolyzation reaction, at last, through condensation with different amine then through condensation with 5-fluoro-1,3-dihydro-indol-2-ono, so we got the targeted production, with an overall yield of 8.1% and 11.2%.