Preparative synthesis of N-acetyl-3-indolinones

Compounds that contain an indole cycle in their structure have biological activity and are a source for the development of new medicinal products. N-acetyl-3-indolinones are actively used as incoming substance for their organic synthesis. Preparative methods for the obtaining of N-acetyl-3-indolinones, used as incoming substances for the synthesis of condensed indole derivatives with high therapeutic activity, have been developed. Synthesis of N-acetyl-3-indolinone was performed by deacetylation and cyclization of N-(2-carboxyphenyl) glycine and its 4-bromo-derivative to form N,O-diacetylindoxyls followed by hydrolysis of the obtained compounds to target indolinones. It was established that brominated derivatives have increased stability as compared with the analogues which do not contain bromine on the benzene ring of the indole nucleus, resulting in the increase in the yield of desired products in the reaction.

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