Vincine and derivatives - with activity in increasing cerebral blood-flow

摘要

The polycyclic indole derivatives claimed are DELTA14-vincine (I), DELTA14-16-epi-vincine (II), and 16-epi-vincine (III) and their acid-addition salts. These cpds. and the known compound vincine, are agents for increasing the cerebral blood flow in man and animals in unit doses of 5-10 mg/kg orally or i.v. LD50 i.v. in mice is between 95 and 180 mg/kg. Extraction of leaves of Craspidospermum verticillatum gives with a solvent e.g. CH2CL2, give (I) and (II). (I) crystallises from hot ethanol. Chromatography on alumina of mother liquord gives (II). Catalytic hydrogenation of (I) gives vincine (IV) and of (II) gives (III).