Process for the preparation of 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide and synthetic intermediates thereof
AssigneeEOS Ethical Oncology S.p.A. Abbreviated Form EOS S.p.A.
InventorsSilvano Spinelli, Valeria Livi
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Abstract
A process for the preparation in high yields and purity of the compound 6-(7-4(1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.
Claims7
Process for the preparation of the compound 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I):
- or a pharmaceutically acceptable salt thereof, comprising reacting a compound of formula (VI):
- wherein R and R′ taken together with the nitrogen atom they are linked to represent a protected primary amino group, with a compound of formula (XVI):
- wherein X is selected from Cl, Br or I in the conditions of the Mitsunobu reaction, to obtain a compound of formula (XII):
- wherein X,R and R′ are as defined above.
Dependencies are inferred from the claim text.