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 kinas e (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 wi th N,N~dimethylformamide dimethyacetal to obtain a N,N-dimethylamidine which is condensed with t-butylcyanoacetate to obtain a N-(2-cyano-2- t~butoxycarbonylvinyl)anthranilate, which is hydrolyzed to yield a N-(2-cyan o- 2~carboxyvinyl)anthranilate followed by decarboxylating to obtain a N-(2-cya no- 2~ carboxyvinyl)anthranilate followed by cyclizing to obtain a 3-cyano-6- alkoxy-7-nitro-4~quinolone.