C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/237.3
C07D 519/04 (2006.01)
Patent
CA 1103664
ABSTRACT OF THE DISCLOSURE This invention as disclosed relates to a process for preparing dione derivatives of Vinca alkaloids, which are dimeric indoledihydroindole dionecompounds of the formula: Formula III Image wherein R is H, C1-C4 alkyl, C3-C4 alkenyl, CH2-CHX-CH3 or CH2-CH2X wherein X is Br or Cl; R2 is H, CH3 or CHO; either one of R3 and R4, when taken singly, is H or OH and the other C2H5 and R5 is H; or R4 and R5, taken together, form an epoxide ring and R3 is C2H5; R7 is Image and R8, taken singly, is H and R9, taken singly, is -O-CH3; or R8 and R9, taken together, are a single bond between C4'' and N3''; and pharmaceutically acceptable acid addition salts thereof. These compounds are useful as anti-tumor agents in mammals, and are also useful as intermediates for the preparation of other anti-tumor vinca alkaloids.
292072
Gutowski Gerald E.
Miller Jean C.
Eli Lilly And Company
Gowling Lafleur Henderson Llp
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