Abstract

Hexafluoroacetone C 1-hydroxyalkylates 1,3,3-trimethyl-3,4-dihydroisoquinoline and its derivatives under the mild conditions in high yields. Similarly to hexafluoroacetone, esters of trifluoropyruvic acid give products of C 1-hydroxyalkylation (II) or lactams (III) depending on the reaction conditions and the nature of R 4-substituent. Reactions of 1,3,3-trimethyl-3,4-hydroisoquinolines with hexafluoroisopropylimines are also investigated. The developed methodes are used to modify Nospani drug. Some aspects of biological activity of the obtained compounds are discussed. ▪

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