Vigilance increasing and psycho-stimulant 10-bromo-vincamine - prepd. e.g. by redn. and rearrangement of 15-bromo-1,2-di:dehydro-3-hydroxy-aspidospermidine-3-carboxylic acid methyl ester

摘要

New vincamine derivs. is 10-bromo-vincamine (I) in optically active or racemic form. (I) and its physiologically tolerable acid addn. salts have vigilance-increasing and psychostimulant activity. Prepn. is by rearrangement of a cpd. (II) (where n is 0 and X is oxygen; or n is 1, X is H and Y is an anion. When n is 0, the rearrangement is carried out in the presence of a reducing agent (pref. triphenylphosphine). The rearrangement can be affected under acidic conditions, 10-epibromovincamine formed as by-product can be converted into (I) by e.g. boiling in xylene with silver or mercury (I) acetate.