PROCESS FOR THE SYNTHESIS OF 3-CYANO-6-ALKOXY-7-NITRO-4-QUINOLINES

摘要

There is provided a process for the preparation of 3-cyano-6-alkoxy-7-nitro-4­-quinolone intermediates useful for the preparation of protein tyrosine kinase (PTK) inhibitors which are useful in the treatment of cancer of the formula, wherein R is alkyl(C,-C3) prepared by reacting a substituted anthranilate with N,N­dimethylformamide dimethyacetal to obtain a N,N-dimethylamidine which is condensed with t-butylcyanoacetate to obtain a N-(2-cyano-2-t­butoxycarbonylvinyl)anthranilate, which is hydrolyzed to yield a N-(2-cyano-2­carboxyvinyl)anthranilate followed by decarboxylating to obtain a N-(2-cyano-2­ carboxyvinyl)anthranilate followed by cyclizing to obtain a 3-cyano-6-alkoxy-7-nitro-4­quinolone.