85573-72-4Relevant articles and documents
2 β - Azidomethyl penicillanic acid dibenzoate. Preparation method of tazobactam intermediate and tazobactam
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Paragraph 0038, (2021/11/21)
The invention provides a preparation method of 2 β -azipenicillanic acid dibenzoate, tazobactam intermediate and tazobactam. The preparation method comprises the following steps: carrying out free radical reaction in a solvent by using a reaction raw material comprising a double-sulfur open-loop compound, a stacked nitrogen source and an oxidant to obtain a product system comprising 2 β - azidomethyl penicillanic acid dibenzoate. By radical addition of the carbon-carbon double bonds of the double-sulfur ring-opening compound through the azide free radical, high-efficiency and high-selectivity synthesis of the disulphide ring-opening compound directly to 2 β - azimaapenem naphthenate is successfully realized through intramolecular radical substitution. Further, 2 β - azidomethyl penicillanic acid dibenzoate is taken as a key intermediate for synthesizing tazobactam, the yield of tazobactam is improved, and the cost is reduced.
Continuous synthesis method of tazobactam intermediate
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Paragraph 0037-0053, (2020/04/22)
The invention provides a continuous synthesis method of a tazobactam intermediate. The device adopted by the continuous synthesis method comprises a continuous reaction device and a heat exchange device, wherein the heat exchange device is used for adjust
Tazobactam intermediate preparation method
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Paragraph 0041-0083, (2019/12/02)
The invention provides a tazobactam intermediate preparation method, which comprises: subjecting benzhydryl penicillanate sulfoxide and 2-mercaptobenzothiazole which are adopted as reaction raw materials to a thermal cracking ring opening reaction at a te
Preparation method of tazobactam
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Paragraph 0031; 0032; 0033, (2019/02/19)
The invention discloses a preparation method of tazobactam. The preparation method comprises the following steps: performing double oxidization on 2beta-chloromethyl penicillanic acid diphenyl methylester by adopting a solution prepared from potassium permanganate, glacial acetic acid and concentrated sulfuric acid; then loading triazole by taking crown ether as a phase transfer catalyst and taking potassium iodide as a catalyst; then performing deprotection to obtain tazobactam. Compared with the prior art, the preparation method disclosed by the invention has the advantages that although sulfur atoms are oxidized into sulfone to lower chlorine atom activity, the use of the crown ether as the phase transfer catalyst and the potassium iodide as the catalyst compensates for the inactivation well. By adopting the method, the stability of the 2beta-chloromethyl penicillanic acid diphenyl methyl ester is improved, the reaction time is shortened, the reaction yield is improved, the operation risk is lowered, and the industrial production is facilitated.
A new approach to the synthesis of tazobactam using an organosilver compound
Xu, Wei Liang,Li, Yun Zheng,Zhang, Qing Shan,Zhu, He Sun
, p. 442 - 446 (2007/10/03)
Tazobactam (9) was synthesized in 8 steps from the readily accessible 6-APA. By the first use of silver triazole as reactant, the formation of the isomer 7 was avoided and a total yield of 50%, which was two to three times higher than that of reported procedures for 9, was obtained. Georg Thieme Verlag Stuttgart.
