89604-92-2Relevant articles and documents
PRODRUG INHIBITORS
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Paragraph 00160; 00162, (2020/10/20)
Provided herein are compounds useful as metallo-β-lactamase (MBL) inhibitors. The compounds have a formula A–B, where A is a β-lactam antibiotic moiety comprising a bridging methylene (-CH2-) covalently attached to -B; and B is a latent MBL inhibitor. Also provided are formulations comprising such compounds; as well as such compounds or formulations for use as a medicament. The compounds and formulations may be used in the treatment of antibiotic resistance, bacterial infection. The compounds and formulations may be used in the inhibition of a bacterial MBL.
Green process for synthesizing ceftazidime side-chain active ester by using microwave-assisted method
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Paragraph 0031-00332, (2018/03/24)
The invention belongs to the technical field of medicines and in particular relates to a green process for synthesizing a ceftazidime side-chain active ester by using a microwave-assisted method. The green process comprises the following steps: by taking a ceftazidime side-chain acid and dithio-bisbenzothiazole as raw materials, and a mixed solution of benzene and acetonitrile as a solvent, under the catalysis of a composite alkali catalyst, dropwise adding triethyl phosphate, performing a microwave-assisted reaction by using a microwave reactor, and performing aftertreatment after the reaction is completed, thereby obtaining a product, wherein the microwave radiation power is 80-300W, and the radiation time is 30-60 minutes. As triethyl phosphate which is low in price is adopted to replace triphenylphosphine which is high in price in the prior art, the production cost can be reduced. The green process for synthesizing the ceftazidime side-chain active ester by using the microwave-assisted method, which is provided by the invention, is low in cost, the production capacity is greatly increased, the yield is increased, that is, up to 97% or greater, the prepared product is relatively high in purity, that is, up to 99% or greater, and a pleasantly surprised technical effect is achieved.
Method for synthesizing 2-Mercaptobenzothiazolyl-(Z)-(2-aminothiazol-4-yl)-2-(tert-butoxycarbonyl) isopropoxyiminoacetate
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Paragraph 0028-0033, (2017/07/21)
The invention relates to a method for synthesizing 2-Mercaptobenzothiazolyl-(Z)-(2-aminothiazol-4-yl)-2-(tert-butoxycarbonyl) isopropoxyiminoacetate and belongs to the technical field of preparation of ceftazidime intermediates. 2-(2-aminothiazole-4-yl)-2-acetic acid and dibenzothiazyl disulfide (DM) are used as raw materials, a dichloromethane and acetonitrile mixed solution serves as a solvent, catalysts pyridine and triethylamine are sequentially added, triethyl phosphite is used as a condensation agent to perform reaction, and suction filtration and drying are performed after reaction is completed to obtain the 2-Mercaptobenzothiazolyl-(Z)-(2-aminothiazol-4-yl)-2-(tert-butoxycarbonyl) isopropoxyiminoacetate. The process is simple, mild in condition, low in cost and high in reaction yield, and the prepared target product is high in quality and purity and suitable for mass production.
A modified procedure for synthesis of the side chain of ceftazidime-activated thioester
Li, Lei,Wang, Guangyuan,Wei, Shanshan,Yan, Xilong,Chen, Ligong
, p. 615 - 620 (2013/07/27)
A modified procedure for synthesis of the side chain of ceftazidime-activated thioester has been established. This key intermediate of ceftazidime was obtained by a more eco-friendly process than conventional methods, and the yield was much higher (up to
