Preparation method of gemifloxacin side chain compound

A technology for gemifloxacin and a compound is applied in the field of preparation of gemifloxacin side chain compounds, can solve problems such as unfavorable industrial production, unfavorable industrial production, low yield and the like, and achieves the effects of low cost, easy realization and simple process
CN113773240BActive Publication Date: 2022-05-31北京阳光诺和药物研究股份有限公司
8 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
北京阳光诺和药物研究股份有限公司
Publication Date
2022-05-31

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention discloses a preparation method of gemifloxacin side chain compound. The preparation method comprises the following steps: S1, 1-N-tert-butoxycarbonyl-4-cyano-3-pyrrolidone reacts with methoxylamine hydrochloride to obtain the compound shown in formula (V); S2, in an inert In the atmosphere, at a temperature of 10-50°C and in the presence of palladium carbon, the compound shown in formula (Ⅴ) is subjected to a hydrogenation reduction reaction for 1-3 hours under a hydrogen atmosphere of 0.1-0.5Mpa; then Boc anhydride is added, and the Continue the hydrogenation reduction reaction at 10-50°C and 0.1-0.5Mpa for 4-8 hours to obtain the compound shown in formula (VI); S3, the compound shown in formula (VI) reacts with an acid to remove the protecting group to obtain Gemifloxacin side chain compound represented by formula (I). The preparation method of the present invention has simple process, very mild reaction conditions, and is easy to realize; (2) the raw material price is low, and the cost is low; (3) a new and effective synthesis process route of gemifloxacin side chain is created.
Need to check novelty before this filing date? Find Prior Art

Description

Preparation method of gemifloxacin side chain compound technical field The present invention relates to a kind of preparation method of gemifloxacin side chain compound, belong to the technical field of pharmaceutical synthesis. Background technique Gemifloxacin is the 4th generation new fluoroquinolone antibacterial agent developed by Korea LG chemical company, as compound Shown in (III): 7-(4-aminomethyl-3-methoxyiminopyrrolidine-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4- Dihydro[1,8]naphthalene-3-carboxylic acid, trade name Factive, has the advantages of good curative effect and less toxic and side effects.

[0003] Gemifloxacin was the first approved treatment for community-acquired disease caused by multidrug-resistant Streptococcus pneumoniae strains (MDRSP). Antibiotics for pneumonia. For the treatment of infections caused by Streptococcus pneumoniae, methicillin-resistant Staphylococcus aureus, Haemophilus influenzae, or Acute bronchitis, chronic bronchitis, ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More