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 formula

wherein
R<2> is CH3 or CHO;
when taken singly, R<5> is H and one of R<3> and R<4> is OH or H and the other is C2H5 and when R<4> and R<5> are taken together, they form an alpha -epoxide ring R<3> is C2H5, when taken singly R<6> is H and R<7> is OR<1> and when R<6> and R<7> are taken together they are =0;
R<1> is H or acetyl; and
R is OCH3 or NH-NH2 with the proviso that if R is -NH-NH2, R<1> is H; or a pharmaceutically acceptable acid addition salt 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-4 beta -hydroxy derivatives.
The compounds are useful as antimitotic agents.