Streptozotocin derivatives and process for preparing the same
Abstract
Abstract METHYL-D-GLUCOSAMINIDE OR A SALT THEREOF IS CONDENSED WITH METHYL ISOCYANATE TO PRODUCE METHYL N-(N''-METHYLCARBAMOYL)-D-GLUCOSAMINIDE WHICH IS THEN TREATED WITH A NITROSO COMPOUND. METHYL N-(N''-NITROSOCARBAMOYL)-DGLUCOSAMINIDE IS PRODUCED. OPTIMALLY, THE CONDENSATION REACTION IS CARRIED OUT IN AN AQUEOUS SOLUTION AND AT A TEMPERATURE OF 50-150*C. WHEN AN ACID ADDITION SALT OF METHYL D-GLUCOSAMINIDE IS EMPLOYED THE CONDENSATION REACTION IS PREFERABLY CARRIED OUT IN THE PRESENCE OF A BASE AND AN AQUEOUS SOLUTION. WHEN NITROUS ACID, AN ALKALI SALT OF NITROUS ACID OR AN ALKYL NITRITE IS EMPLOYED AS THE NITROSO COMPOUND THE TREATMENT WITH THE NITROSO COMPOUND IS CARRIED OUT PREFERABLY IN THE PRESENCE OF AN ACID AND AT A TEMPERATURE OF -5 TO 10*C. THE COMPOUNDS OF THE INVENTION EXERT A TUMOR INHIBITORY EFFECT ON MICE AND RATS. THEY ARE SUBSTANTIALLY FREE OF DIABETOGENIC SIDE EFFECTS.
Inventors
- 👤 T Suami
- 👤 T Machinami
Bibliographic Details
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