- Synthetic method of furazolidone metabolite AOZ
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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.
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Paragraph 0028; 0031
(2020/07/13)
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- 6- or 7-beta-[2-[4-(substituted)-2,3-dioxopiperazin-1-yl) carbonylamino]-(substituted)acetamido]-penicillin and cephalosporin derivatives
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Antibacterial agents have the formula (I) or are pharmaceutically acceptable salts or invivohydrolysable esters thereof: in which Y1 is oxygen, sulphur or -CH2 and Z represents hydrogen, halogen, C1-4alkoxy, -CH2-Q or -CH=CH-Q where Q represents hydrogen, halogen, hydroxy, mercapto, cyano, carboxy, carboxylic ester, C1-4alkyloxy, acyloxy, aryl, a heterocyclyl group bonded via carbon, a heterocyclylthio group or a nitrogen containing heterocyclic group bonded via nitrogen;, R5 represents phenyl, substituted phenyl, cyclohexenyl, cyclohexadienyl or an optionally substituted 5 or 6-membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphur or nitrogen, R6 is hydrogen, hydroxymethyl, formamido, or methoxy, R7 and R8 are the same or different and represent hydrogen, C1-6alkyl, substituted C1-6alkyl, halogen, amino, phenyl, substituted phenyl, hydroxy or C1-6alkoxy or R7 and R8 form the residue of an optionally substituted 5 or 6- membered carbocyclic ring or a 5 or 6-membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphur or nitrogen, R9 is wherein R10 and R11 are the same or different and each represents hydroxy, or protected hydroxy and XR9 is -(CH2)nR9, -NHCOR9, -N=CHR9, -NHCH2R9, or -COR9, where n is from 0 to 2; with the proviso that XR9 does not represent -N=CHR9 when R6 represents hydrogen. The use of the compounds is described together with intermediates for their preparation.
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