Method for preparation of 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(aS,7aS)-octahydro-6H-pyr- rolo[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid

Patent No. 9,556,173

Issued: January 31, 2017
Filed: June 5, 2013
PCT Filed: June 05, 2013
PCT No.: PCT/UA2013/000055
371(c)(1),(2),(4) Date: January 27, 2016
PCT Pub. No.: WO2014/185881
PCT Pub. Date: November 20, 2014

Inventor: Derkach; Nataliia Mykolaivna (Kiev, UA)


This invention relates to methods for preparation of chemical compound 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4aS,7aS)-octahydro-6H-py- rrolo[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid, which comprise addition of heterocyclic amine containing protecting group, to ethyl-3-oxo-3-(2,4,5-trifluoro-3-methoxyphenyl)propanoate, followed by interaction with triethyl orthoformate, addition of cyclic amine, subsequent cyclization and formation of target product. The method for preparation claimed is technologically simple in comparison with analog and requires no special complex technical operations, which in its turn simplifies method for preparation of this chemical compound, and reduces cost of the final product, while the commercial production utilizing the method claimed has low degree of environmental threat.


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