| Vascular endothelial growth factor (VEGF) plays an important role in the formation of tumor angiogenesis by promoting the formation of new blood vessels, and the proliferation and differentiation of tumor cells can promote the proliferation and differentiation of tumor cells.In recent years, it has been found that tyrosine kinase VEGFR-2 is a key target for anti-cancer drugs, so VEGFR-2 tyrosine kinase inhibitors have become an important direction in the research of anticancer drugs.The purpose of this study is connected to the synthesis of urea based 2-indolinone-benzimidazole derivatives, obtained by screening with active and independent intellectual property rights of the compounds, for further study on the activity. This study is mainly carried out in the following aspects of the work:1 The new structure, no reports of novel VEGFR-2 tyrosine kinase inhibitor had been designed for retrosyntheticanalysis. Considering of the reaction feasibility, route complexity and operational safety, designed reasonable synthetic route for every compound.2 Each compound is synthesized according to the synthetic route design. Indolin-2-one,5-methylindolin-2-one,6-methylindolin-2-one,7-methylindolin-2-one, 5-chloroindolin-2-one,7-chloroindolin-2-one,5-bromoindolin-2-one are synthesized. 3-Aminoindolin-2-one,3-amino-5-methylindolin-2-one,3-amino-6-methylindolin-2-one,3-amino-7-methylindolin-2-one,3-amino-5-chloroindolin-2-one,3-amino-7-chl-oroindolin-2-one,3-amino-5-bromoindolin-2-one are synthesized.2-Aminobenzimida-zole,2-aminomethyl benzimida-zole,2-benzimidazole amide,5-methyl-2-aldehyde benzimidazole 1-methyl-2-amine methyl benzimidazole are synthesized.3 The compounds were synthesizedby indolin-2-one and benzimidazole, connected by urea. 1-((1H-benzo[d]imidazol-2-yl)methyl)-3-phenylurea and 1-((1H-benzo[d]imidazol-2-yl)methyl)-3-(2-oxoindolin-3-yl)urea were synthesized. The two amino of 2-oxindoles and benzimidazole were protected, which is explored. |
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