abstract |
A PROCESS FOR PREPARING THE 9-AMINO CAMPTOTHECIN OF (FORMULA 1)SAID PROCCES COMPRISING :(1) REACTING A COMPOUND OF FORMULA (111)WHEREIN THE HYDROXY GROUP ON RING A IS IN THE 10- OR 12- POSITION, WITH A NITRATING AGENT, SO OBTAINING A CORRESPONDING COMPOUND OF FORMULA (1V)(2) CONVERTING THE COMPOUND OF FORMULA (IV) INTO A CORRESPONDING COMPOUND OF FORMULA (V)WHERE X0 IS A GROUP THAT CAN BE REMOVED REDUCTIVELY; AND (3) REDUCTIVELY REMOVING THE SAID X0 GROUP AND REDUCING THE NITRO GROUP OF THE COMPOUND OF FORMULA (V), SO OBTAINING THE 9- AMINO CAMPTOTHECIN OF FORMULA (I), A KNOWN ANTITUMOR COMPOUND. THE PRESENT INVENTION INCLUDES ALSO IN ITS SCOPE COMPOUND HAVING THE ABOVE REPORTED FORMULA (V) AND COMPOUND OF FORMULA (VII)WHICH ARE ENDOWED WITH ANTITUMOR ACTIVITY. |