76646-91-8Relevant articles and documents
A versatile strategy for the solid-phase synthesis of penicillin derivatives: Efficient preparation of 2β-methyl substituted penams as β-lactamase inhibitor analogues
Boggian, Dora B.,Mata, Ernesto G.
, p. 3397 - 3404 (2006)
A convenient solid-phase method for the synthesis of 2β-methyl substituted penicillins using commercially available resins is described. Functionalization of Merrifield and Wang resin bound penam derivatives was performed by penicillin sulfoxide rearrangement and the products were released from the supports under mild conditions. The utility of this methodology has been demonstrated by synthesizing a small library of penicillin derivatives in moderate to very good overall isolated yields for the multistep synthetic sequence. Georg Thieme Verlag Stuttgart.
Synthesis method of sulbactam
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Paragraph 0027; 0029; 0031; 0033; 0035; 0037, (2020/11/02)
The invention relates to a synthesis method of sulbactam, and belongs to the field of beta-lactamase inhibitor synthesis. In the method, 6-aminopenicillanic acid (6-APA) as a raw material is dissolvedin an organic solvent, and is adopted together with bromine as substrates under a strong acid condition, 6,6-dibromo penicillanic acid is formed through diazotization bromination in a manner of dropwise adding a sodium nitrite solution, and then one-step oxidation and reduction are performed to obtain sulbactam. According to the method, a hydrogen peroxide one-step oxidation mode is adopted, andthe use of potassium permanganate is avoided from the source, so that the generation of waste salt is reduced, and meanwhile, the use of a large amount of ethyl acetate is avoided. The method not onlyreduces the emission of three wastes from the source and greatly reduces the emission of organic matters and waste salt in the original process, but also greatly reduces the side reaction and the rawmaterial cost.
Method for preparing sulbactam acid
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Page/Page column 5-11, (2019/05/15)
The invention relates to the field of pharmaceutical synthesis and provides a method for preparing sulbactam acid. The method is used for solving the problem of the traditional synthesis methods thatthe yield is low. The method comprises the following steps: S1. diazotation and bromination reaction: adding bromine, a dilute sulfuric acid solution and sodium nitrite solids into 6-aminopenicillanicacid, so as to obtain a first intermediate, wherein the dilute sulfuric acid solution adopts depleted deuterium water as a solvent; S2. oxidation reaction: dropwise adding potassium permanganate anda dilute sulfuric acid solution into the first intermediate, so as to obtain a second intermediate; and S3. hydrogenation reaction: add strontium powder and a dilute sulfuric acid solution into the second intermediate, thereby obtaining a product, i.e., the sulbactam acid, wherein the dilute sulfuric acid solution adopts depleted deuterium water as a solvent. Through preparing the dilute sulfuricacid solution by adopting the depleted deuterium water as the solvent and adopting the strontium powder as a catalyst, the improvement on reaction activity of dilute sulfuric acid is facilitated, theconversion ratio of reaction is increased, and thus, the increase of reaction yield is facilitated, so that the yield of reaction can be higher than 90%.
Sulbactam sodium compound containing one-twentieth water and pharmaceutical composition thereof
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Paragraph 0030; 0032; 0038; 0040; 0046; 0048, (2019/01/23)
The invention discloses a sulbactam sodium compound containing one-twentieth water. The sulbactam sodium compound is white crystalline powder, and each mole of sulbactam sodium contains one-twentiethmole of water. The sulbactam sodium compound has main diffraction peaks at the positions with the corresponding main X-ray characteristic diffraction peak 2 theta angle of 14.23+/-0.2 degrees, 17.76+/-0.2 degrees, 19.22+/-0.2 degrees, 23.09+/-0.2 degrees, 24.60+/-0.2 degrees and 27.86+/-0.2 degrees. The sulbactam sodium compound prepared by means of a method has high stability and meets the requirements for being used a raw material of a preparation.