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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。
In order to better control the quality of leremyramide, three kinds of degradation impurities of lemetilamine were designed and synthesized. (S) -N- [2- (4-hydroxy-2,6,7,8-tetrahydro- lH-indeno [5,4-b] furan-8- yl) ethyl] propanamide IP1), 2-hydroxy-N- [2- [(S) -2,6,7,8- tetrahydro- lH-indeno [5,4- b] furan- 8-yl] ethyl] (IP2) and N- [2- (2,6- dihydro-lH-indeno [5,4-b] furan- 8-yl) ethyl] propanamide (IP3) (13) CNMR and HRMS confirmation structure. Destructive tests show that acidic conditions mainly produce impurities IP1 and IP3, oxidation conditions mainly produce impurities IP2.