185225-84-7Relevant articles and documents
Sitafloxacin three membered ring intermediate preparation method
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Paragraph 0038-0064, (2017/07/07)
The invention discloses a preparation method for a three-membered ring intermediate of sitafloxacin hydrate. The preparation method comprises the following steps: dimethyl malonate and 1,1,2-tribromo-2-fluoroethane react to synthesize a solid A, the solid A is subjected to debromination to prepare an oily liquid B, the oily liquid B is subjected to branched chain removal to prepare a solid C, the solid C is hydrolyzed to prepare a solid D, the solid D is subjected to chiral resolution with L-leucinamide and reduced to prepare a solid F, the solid F is introduced to an amino group and combined with p-toluenesulfonic acid to prepare the three-membered ring intermediate of sitafloxacin hydrate. The preparation method has fewer steps for preparing the three-membered ring intermediate of sitafloxacin hydrate, unnecessary isomer is separated by one step with the chiral resolution method, the product yield and purity are higher, and scale production is easier.
Stereoselective synthesis of cis -2-fluorocyclopropanecarboxylic acid
Shibue, Taku,Fukuda, Yasumichi
, p. 7226 - 7231 (2014/08/18)
A rhodium-catalyzed cyclopropanation of 1-fluoro-1-(phenylsulfonyl)ethylene and diazo esters is described as an effective method for the stereoselective synthesis of cis-2-fluorocyclopropanecarboxylic acid. This process provides an example of the cyclopro
Synthetic studies on the key component of the new generation of quinolonecarboxylic acid, DU-6859. 1. Synthesis of (1R,2S)-2-fluorocyclopropylamine by the use of optical resolution
Tamura, Osamu,Hashimoto, Masaru,Kobayashi, Yuko,Katoh, Tadashi,Nakatani, Kazuhiko,Kamada, Masahiro,Hayakawa, Isao,Akiba, Toshifumi,Terashima, Shiro
, p. 3889 - 3904 (2007/10/02)
The title synthesis was achieved by employing highly cis-selective cyclopropanation of N-benzyl-N-vinylcarbamates with zinc-monofluorocarbenoid, deprotection of the formed N-benzyl-N-(cis-2-fluorocyclopropyl)carbamates, and optical resolution of the resul