雷美替胺降解杂质的制备

发布时间：2018-10-12 07:27

【摘要】：为了更好地控制雷美替胺的质量,设计并合成了雷美替胺的3种降解杂质。分别为(S)-N-[2-(4-羟基-2,6,7,8-四氢-1H-茚并[5,4-b]呋喃-8-基)乙基]丙酰胺(IP1)、2-羟基-N-[2-[(S)-2,6,7,8-四氢-1H-茚并[5,4-b]呋喃-8-基]乙基]丙酰胺(IP2)和N-[2-(2,6-二氢-1H-茚并[5,4-b]呋喃-8-基)乙基]丙酰胺(IP3),所得产物经~1HNMR、~(13)CNMR和HRMS确证结构。破坏性试验证明,酸性条件主要产生杂质IP1与IP3,氧化条件下主要产生杂质IP2。
[Abstract]:In order to better control the quality of remetidine, three kinds of degradation impurities were designed and synthesized. The products are (S) N- [2- (4-hydroxy-2oxy) -7- (tetrahydro-8-) -1H-indeno [54-b] furan-8- ethyl] propionamide (IP1), 2-hydroxy-N- [2- [(S) -2o _ 6N _ (7H) -tetrahydro-1H-) and [54-b] furan -8indenyl] ethyl] propionamide (IP2), respectively, and N- [2- (2- (2o 6- dihydro-1H-) and [54-b] furan-8-) ethyl] propionamide (IP3), respectively. The obtained products are as follows: N- [2- (2-) -dihydro-1H- and [54-b] furan-8-) ethyl] propionamide (IP3). The structure was confirmed by ~ 1HN MR13 CNMR and HRMS. The destructive test shows that the main impurity IP1 is produced under acidic condition and the impurity IP2. is produced under the condition of IP3, oxidation.
【作者单位】：扬子江药业集团有限公司;
【分类号】：R943

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