摘要
目的为了加强对利奈唑胺注射液的质量控制,合成了口恶唑烷酮类抗生素利奈唑胺的两个特定杂质。方法以利奈唑胺为起始原料,经水解制备得到降解杂质(2S)-1-氨基-3-{[3-氟-4-(4-吗啉基)苯基]氨基}-2-丙醇,再经Boc保护、乙酰化、脱Boc制得降解杂质N-[(2S)-3-氨基-2-羟基丙基]-N-[3-氟-4-(4-吗啉基)苯基]-乙酰胺。结果与结论合成的两种降解杂质的结构经1H-NMR、MS确证,可以作为利奈唑胺注射液质量控制的杂质对照品。
The degradation impurits of ox azolidinone antibiotic linezolid, （ 2 S ） - 1 - amino -3 - （ 3 - fluoro -4- morpholinophenylamino） propan-2-ol （ 2 ） and N- [ （2S） - （3-amino-2-hydroxypropyl） -N- （ 3-fluoro-4- morpholinopenyl ）acetamide （5） were easily found in the process of high-temperature sterilization and long-term placement. In order to perform the quality control of linezolid injection, impurity 2 was hydrolyzed from linezolid and impurity 5 was synthesized in three steps by Boc protection, acetylation and Boc deprotection from impurity 2. The structures were confirmed by MS, ^1H-NMR and ^13 C-NMR. The two specified impurities can be used as the reference substance of the related substances in the quality control of Linezolid injection.
出处
《中国药物化学杂志》
CAS
CSCD
2015年第2期125-128,共4页
Chinese Journal of Medicinal Chemistry
基金
上海市青年科技启明星计划项目(12QB1404800)
关键词
利奈唑胺
降解杂质
合成
linezolid
degradation impurities
synthesis
