Oxazolidinedione derivatives of Vinca alkaloids

Abstract

3-Spiro-5"-oxazolidine-2",4"-dione derivatives of Vinca alkaloids, useful as anti-tumor agents and as intermediates.

We claim: 
     
       1. A compound of the formula ##STR5## wherein R is H, C 1  -C 4  alkyl; C 3  -C 4  alkenyl, CH 2  --CHX--CH 3  or CH 2  --CH 2  X; wherein   X is Br or Cl;   R 1  is OH, ##STR6## R 2  is H, CH 3  or CHO; one of R 3  and R 4 , when taken singly, is H or OH and the other C 2  H 5  ;   R 5 , when taken singly, is H;   and R 4  and R 5 , when taken together, form an epoxide; and pharmaceutically-acceptable salts thereof.   
     
     
       2. A compound according to claim 1, said compound being VLB 3"-methyl-3-spiro-5"-oxazolidine-2",4"-dione. 
     
     
       3. The sulfate salt of the compound of claim 2. 
     
     
       4. A compound according to claim 1 said compound being VLB 3"-(β-chloroethyl)-3-spiro-5"-oxazolidine-2",4"-dione. 
     
     
       5. The sulfate salt of the compound of claim 4. 
     
     
       6. A compound according to claim 1 wherein R 1  is OH. 
     
     
       7. A compound according to claim 1 wherein R 1  is ##STR7##