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Tosufloxacin tosylate and preparation method thereof

A technology of tosufloxacin tosylate and tosufloxacin tosylate, which is applied in the field of medicine, can solve problems such as low yield, low purity, and no ideal synthesis route of tosufloxacin tosylate, and achieve high yield The effect of high and low impurity content

Pending Publication Date: 2022-04-19
赤峰万泽药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The invention provides a kind of tosufloxacin tosylate and its preparation method to solve the problem that there is no ideal synthesis route of tosufloxacin tosylate in the prior art and tosufloxacin tosylate prepared by the existing method Problems such as high impurity content, low purity, and low yield

Method used

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  • Tosufloxacin tosylate and preparation method thereof
  • Tosufloxacin tosylate and preparation method thereof
  • Tosufloxacin tosylate and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0033] This embodiment provides a preparation method of tosufloxacin tosylate. The preparation method of tosufloxacin tosylate of the present embodiment may further comprise the steps:

[0034] Amination: Tosufloxacin tosylate amine was prepared by amination reaction using acetic anhydride, triethyl orthoformate, fluclonicotinate, methanol, and 2,4-difluoroaniline as starting materials;

[0035] Cyclization: based on tosufloxacin tosylate amine, prepare tosufloxacin tosylate cyclic compound through cyclization reaction;

[0036] Substitution: Based on the tosufloxacin tosylate cyclic compound, the tosufloxacin tosylate substituted was prepared through a substitution reaction;

[0037] Hydrolysis into salt: Based on the tosufloxacin toluenesulfonate substitute, the crude product of tosufloxacin toluenesulfonate is prepared by hydrolysis into salt, and the refined tosufloxacin toluenesulfonate is obtained.

[0038] In this example, tosufloxacin tosylate amine is 1-(2,4-difluor...

Embodiment 2

[0093] This embodiment provides a kind of tosufloxacin tosylate and its preparation method. The same technical features of the preparation method of this embodiment and embodiment 1 will not be repeated, and only the difference with embodiment 1 will be described:

[0094] (1) Tosufloxacin tosylate amination post:

[0095] Reaction process: in the present embodiment, the charging capacity of fluchloronic acid ester is 300.0kg (1.0714kmol), the charging capacity of acetic anhydride is 270.0kg (2.6447kmol), the charging capacity of triethyl orthoformate is 225.0kg ( 2.4433kmol), the feeding amount of 2,4-difluoroaniline is 153.75kg (1.4914kmol), and the feeding amount of methanol is 900.0kg (28.0899kmol).

[0096] The reaction process comprises the following steps: use a vacuum pump to sequentially draw acetic anhydride and triethyl orthoformate into the reaction tank from the liquid feed port, start stirring, add fluchloronicotinic acid ester from the solid feed port, after th...

Embodiment 3

[0115] This embodiment provides a kind of tosufloxacin tosylate and its preparation method. The same technical features of the preparation method of this embodiment and embodiment 1 will not be repeated, and only the difference with embodiment 1 will be described:

[0116] (1) Tosufloxacin tosylate amination post:

[0117] Reaction process: In the present embodiment, the feeding amount of fluchloronic acid ester is 200kg, the feeding amount of acetic anhydride is 180kg, the feeding amount of triethyl orthoformate is 150kg, and the feeding amount of 2,4-difluoroaniline is 102.5kg, the feeding amount of methanol is 600kg.

[0118] The reaction process comprises the following steps: use a vacuum pump to sequentially draw acetic anhydride and triethyl orthoformate into the reaction tank from the liquid feed port, start stirring, add fluchloronicotinic acid ester from the solid feed port, after the feeding is completed, seal the tank, and the temperature rises to 120°C, reflux re...

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Abstract

The invention provides tosufloxacin tosylate and a preparation method thereof, and the preparation method comprises the following steps: taking acetic anhydride, triethyl orthoformate, fluorine chloronicotinate, methanol and 2, 4-difluoroaniline as initial raw materials, and carrying out amination reaction to prepare tosufloxacin tosylate amido; based on the amino substance, preparing a tosufloxacin tosylate cyclization compound through cyclization reaction; preparing a tosufloxacin tosylate substitute through a substitution reaction on the basis of the cyclization compound; based on the substitutes, preparing a tosufloxacin tosylate crude product through a hydrolysis salt-forming reaction, and refining to obtain tosufloxacin tosylate. The preparation method covers all steps of a tosufloxacin tosylate synthesis route, a complete production chain is formed by designing all the steps of the synthesis route, and the prepared tosufloxacin tosylate is low in impurity content, high in purity and high in yield and meets the high-quality requirement of the medicine field for medicines.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular tosufloxacin tosylate and a preparation method thereof. Background technique [0002] Tosufloxacin tosylate is a new type of synthetic quinolone broad-spectrum antibacterial drug, which has the characteristics of strong antibacterial activity, broad antibacterial spectrum, low toxicity, and small side effects. It is effective against Gram-positive bacteria, Gram-negative bacteria, Anaerobic bacteria, chlamydia, mycoplasma, etc. have strong antibacterial effects. Tosufloxacin tosylate has a wide range of clinical applications and can be used for upper and lower respiratory tract infections, acute and chronic bronchitis, bronchiectasis, pneumonia, and urogenital infections caused by sensitive bacteria. systemic infection, biliary tract infection and intestinal infection. [0003] The synthetic route of tosufloxacin tosylate is relatively complicated, and there is no ideal synthetic ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04C07C309/30C07C303/32C07C303/44C07D213/61
CPCC07D471/04C07C309/30C07C303/32C07C303/44C07D213/61
Inventor 张海立郭振军刘海涛
Owner 赤峰万泽药业股份有限公司
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