Cerebrovascular desoxy-vincaminic amide prepn. - from tabersonine, by conversion to an amide, oxidative rearrangement and reduction

摘要

Desoxy vincaminic amides (I) are prepd. from tabersonine (II), by conversion to tabersoninic acid (III) then to its amide (IV), oxidative rearrangement and hydrogenation. In the formulae, either R' and R" are H, alkyl, phenyl-alkyl, cycloalkyl or cycloalkylalkyl, the alkyl gps. having 1-4C or R'NR" form a heterocycle having 4-6C atoms and/or another hetero O, N or S atom, and which may have an alkyl gp. on the other N atom. Amides (I) are known cerebrovascular agents. A typical prod. is (beta S, 14R, 16S)-desoxy-vincaminamide.