PROCESS FOR PREPARING THE ANTI-TUMOR AGENT 6-(7-((1-AMINOCYCLOPROPYL)METHOXY)-6-METHOXYQUINOLIN-4-YLOXY)-N-METHYL-1-NAPHTHAMIDE AND ITS CRYSTALLINE

摘要

The present invention relates a new process to synthesize 6-(7-((l-aminocyclo-propyl)- methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl- l -naphthamide (AL3810) by deprotection of substituted benzyl 1 -((6-methoxy-4-(5-(methylcarbamoyl)naphthalen-2-yloxy)quinolin-7-yloxy)- methyl)cyc-lopropylcarbamate (Formula I) under a diluted or weak acidic condition. A stable crystalline form of 6-(7-((l-aminocyclo-propyl)-methoxy)-6-methoxyquinolin-4-yloxy)-N- methyl- 1 -naphthamide has also been prepared.