80-65-9Relevant articles and documents
Preparation method and application of 3-amino-2-oxazolidinone derivative
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Paragraph 0070-0074, (2021/04/10)
The invention discloses a preparation method and application of a 3-amino-2-oxazolidinone derivative. The invention relates to a derivative of a general formula I with a bacterial quorum sensing regulation effect, wherein definitions of substituent groups in the general formula I are described in the specification; a preparation method of the compound of general formula I; a pharmaceutical composition comprising the compound of general formula I; and application of the compound of general formula I in the preparation of medicaments. Biological activity detection is carried out on the compound shown as the general formula I, the regulation effect of the compound shown as the general formula I on bacterial quorum sensing is further proved, an experimental basis is provided for a new strategy for treating diseases caused by drug-resistant gram-negative bacteria, and an important research value is achieved for solving the drug resistance problem.
Synthetic method of furazolidone metabolite AOZ
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Paragraph 0022; 0026, (2020/07/13)
The invention discloses a preparation method of 3-amino-2-oxazolidinone (AOZ). The method comprises the following steps: 1) carrying out a reaction on ethylene glycol and PBr3 to obtain 2-bromoethanol; 2) carrying out a substitution reaction on 2-bromoethanol and an alkali, then adding hydrazine hydrate into the system, continuously carrying out a ring-opening reaction, and removing excessive 2-bromoethanol and water after the reaction is completed to obtain an intermediate 2-hydrazinoethanol; and 3) in the presence of an alkali, carrying out a reaction on 2-hydrazinoethanol and diethyl carbonate to obtain 3-amino-2-oxazolidinone (AOZ). According to the method, a nitrofuran metabolite AOZ is synthesized by adopting a one-pot method at the rear half part, so that the loss of a separated andpurified sample in the synthesis process is greatly reduced.
Synthetic method of furazolidone metabolite AOZ
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Paragraph 0028; 0033, (2020/07/13)
The invention discloses a preparation method of 3-amino-2-oxazolidinone (AOZ). The method comprises the following steps: 1) carrying out a reaction on ethylene glycol and PBr3 to obtain 2-bromoethanol; 2) in the presence of an alkali, carrying out a reaction on NH2NH2Boc and 2-bromoethanol to obtain Boc protected 2-hydrazinoethanol; 3) in the presence of an alkali, carrying out a reaction on Boc protected 2-hydrazinoethanol and diethyl carbonate to obtain Boc protected 3-amino-2-oxazolidinone; and 4) performing deprotection on the Boc group in the Boc protected 3-amino-2-oxazolidinone to obtain 3-amino-2-oxazolidinone. According to the method, the yield of AOZ in the synthesis process is obviously increased, and separation and purification are facilitated.