Vincaleukoblastine derivatives, a process for their preparation, pharmaceutical formulations containing them and the derivatives for use as antimitotic agents

摘要

Vincaleukoblastine derivates of the formulawhereinR² is CH₃ or CHO;when taken singly, R⁵ is H and one of R³ and R⁴ is OH or H and the other is C₂H₅ and when R⁴ and R⁵ are taken together, they form an a-epoxide ring R³ is C₂H₅, when taken singly R⁶ is H and R' is OR' and when R⁶ and R' are taken together they are =0;R¹ is H or acetyl; andR is OCH, or NH-NH₂ with the proviso that if R is -NH-NH₂, R¹ is H; or a pharmaceutically acceptable acid addition saft thereof, are prepared by reduction of the corresponding 4-desacetoxy-4-oxo derivatives which in turn were prepared by the oxidation of the corresponding 4- desacetyl-4β-hydroxy derivatives.;The compounds are useful as antimitotic agents.