898543-06-1
898543-06-1 結(jié)構(gòu)式
基本信息
利伐沙班中間體5
利伐沙班雜質(zhì)27
利伐沙班雜質(zhì) 7-2
利伐沙班 中間體 R-7.2
4-[4-[(5S)-5-(氨基甲基)-2-氧代-3-惡唑烷...
(S)-4-(4-(5-(氨基甲基)-2-氧代惡唑烷-3-基)苯基)嗎啉-3-酮鹽酸鹽
4-[4-[(5S)-5-(氨甲基)-2-氧代-3-惡唑烷基]苯基]-3-嗎啉酮鹽酸鹽
4-[4-[(5S)-5-(氨甲基)-2-羰基-3-唑烷基]苯基]-3-嗎啡啉酮鹽酸鹽
(S)-4-(4-(5-(氨基甲基)-2-氧代噁唑烷-3-基)苯基)嗎啉-3-酮鹽酸鹽
Rivaroxaban Impurity 7-2
Rivaroxaban interMediate A
4-{4-[(5S)-5-aMinoMethyl)-2-oxo-1,3-oxazolidin-3-yl}Morpholin-3-one
(S)-4-(4-(5-(Aminomethyl)-2-oxoxazolidin-3-yl)phenyl)morpholin-3-one.HCl
(S)-4-(4-(5-(Aminomethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one.HCl
4-(4-(5-(Aminomethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one hydrochloride
(S)-4-(4-(5-(aMinoMethyl)-2-oxooxazolidin-3-yl)phenyl)Morpholin-3-one hydrochloride
4-{4-[(5S)-5-aMinoMethyl)-2-oxo-1,3-oxazolidin-3-yl} Mor-pholin -3-one hydrochloride
4-[4-[(5S)-5-(Aminomethyl)-2-oxo-3-oxazolidinyl]phenyl]-3-morpholinone hydrochloride
物理化學(xué)性質(zhì)
制備方法
446292-08-6
898543-06-1
以2-[[(5S)-2-氧代-3-[4-(3-氧代-4-嗎啉基)苯基]-5-噁唑烷基]甲基]-1H-異吲哚-1,3(2H)-二酮為原料，合成(S)-4-(4-(5-(氨基甲基)-2-氧代噁唑烷-3-基)苯基)嗎啉-3-酮鹽酸鹽的一般步驟如下：在四頸圓底燒瓶中，加入甲醇（2900 mL），2-[[(5S)-2-氧代-3-[4-(3-氧代-4-嗎啉基)苯基]-5-噁唑烷基]甲基]-1H-異吲哚-1,3(2H)-二酮（290 g）和40%甲胺水溶液（265 g）。將反應(yīng)混合物在25至30℃下攪拌1小時(shí)，隨后加熱至60至65℃，并在該溫度下維持4小時(shí)。反應(yīng)完成后，將混合物冷卻至25至30℃，加入濃鹽酸（290 mL，調(diào)節(jié)pH至1-2），繼續(xù)攪拌30分鐘。過濾收集所得固體，并用冷甲醇（290 mL）洗滌。產(chǎn)率為92.0%。
參考文獻(xiàn)：
[1] Patent: WO2014/102820, 2014, A2. Location in patent: Paragraph 059
[2] Patent: CN105085371, 2017, B. Location in patent: Paragraph 0102-0104
[3] Patent: CN105085431, 2017, B. Location in patent: Paragraph 0093; 0094; 0095; 0096; 0097; 0098; 0099
[4] Patent: WO2012/35057, 2012, A2. Location in patent: Page/Page column 29
[5] Patent: WO2013/121436, 2013, A2. Location in patent: Page/Page column 27