6937-15-1Relevant articles and documents
Method of preparing linezolid
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Paragraph 0048; 0049; 0050, (2018/04/02)
The invention relates to a method of preparing an oxazolidine antibacterial agent-linezolid. The method includes: enabling (S, E)-N-benzal-1-(ethylene oxide-2-group)-methylamine and morpholino fluoro-phenyl carbamate to react in a non-nucleophilic agent under action of alkali and catalyst to obtain a high-purity imine intermediate; subjecting the intermediate to hydrolysis and acylation to generate linezolid. The method is high in yield, simple to operate, mild in reaction condition and suitable for industrial production.
Method for preparing 3-hydroxyazetidine hydrochloride and tert-butyl 3-hydroxyazetidine-1-carboxylate
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Paragraph 0048; 0049; 0050, (2017/08/30)
The invention discloses a method for preparing 3-hydroxyazetidine hydrochloride and tert-butyl 3-hydroxyazetidine-1-carboxylate and relates to the field of drug synthesis. The method comprises the following steps: taking 3-sustituted-1,2-epoxypropane, a benzaldehyde compound and ammonium hydroxide as initiators so as to obtain a first intermediate with an imine structure; and hydrolyzing the first intermediate so as to obtain hydroxylammonium salt, and performing ring closing, thereby obtaining the target product. On the basis of the preparation method, two different synthetic strategies of sequentially performing ring closing and introducing a Boc group and sequentially introducing the Boc group and performing ring closing are respectively adopted from the hydroxylammonium salt, and then tert-butyl 3-hydroxyazetidine-1-carboxylate is prepared at high efficiency. According to the previous three preparation methods, the harsh conditions that a Pd/C catalyst and hydrogen are used and the like are avoided, and extra process steps are avoided. The whole process flow is reasonable in design, and the method is mild in conditions, simple and convenient to operate, readily available in raw materials, high in production efficiency and very suitable for large-scale industrial production.
4-Benzoylamino-3-hydroxybutyric acid, historically first "anomalous racemate": Reinvestigation
Bredikhin, Alexander A.,Bredikhina, Zemfira A.,Zakharychev, Dmitry V.,Samigullina, Aida I.,Gubaidullin, Aidar T.
supporting information, p. 1362 - 1373 (2015/05/20)
Chiral 4-benzoylamino-3-hydroxybutyric acid (1) was recognized in 1930 as the first example of "anomalous racemates" (correct to say, anomalous conglomerates), that is, specific addition compounds formed by different enantiomers in unequal ratio. Through the comparative (racemic against homochiral samples) inspection of the IR spectra, single crystal X-ray diffraction, PXRD analysis, and solubility data we have found that this substance forms normal racemic compound in the solid state, and must be excluded from the very short list of anomalous conglomerates. At the same time homo-1 is dissolved in 25 times better than rac-1, and this feature belongs to another interesting and rare type, namely, "anticonglomerates". Some of the reasons for this behavior are discussed.
