143062-84-4Relevant 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.
Synthesis of cis-2-fluorocyclopropylamine by stereoselective cyclopropanation under phase-transfer conditions
Matsuo, Jun-Ichi,Tani, Yu-Ichirou,Hayakawa, Yu-Ichirou
, p. 464 - 465 (2007/10/03)
cis-2-Fluorocyclopropylamine is stereoselectively synthesized by cyclopropanation of 3-aryl-2-vinyl-3-(methoxy)isoin-dol-1-one by treating dibromofluoromethane with saturated aqueous KOH solution in the presence of 18-crown-6 in dichloromethane, followed by removal of a bromine atom of the formed bromofluorocyclopropane derivative with Raney Ni, and successive three steps-deprotection procedures for generating an amino group on the cyclopropane ring.
Synthetic Studies on the Key Component of the New Generation of Quinolonecarboxylic Acid, DU-6859. 2. Asymmetric Synthesis of (1R,2S)-2-Fluorocyclopropylamine
Akiba, Toshifumi,Tamura, Osamu,Hashimoto, Masaru,Kobayashi, Yuko,Katoh, Tadashi,et al.
, p. 3905 - 3914 (2007/10/02)
The title synthesis was achieved by featuring diastereoface-selective cyclopropanation of (4R,5S)-4,5-diphenyl-3-vinyl-2-oxazolidinone and its related compounds, the chiral conformationally rigid N-vinylcarbamates, with zinc-monofluorocarbenoid, followed