137973-76-3
137973-76-3 结构式
基本信息
托伐普坦杂质5(DM-21826)
7-氯-1-[2-甲基-4-[(2-甲基苯甲酰)氨基]苯甲酰
N-(4-(7-氯-5-氧代-2,3,4,5-四氢-1H-苯并[B]氮杂-1-羰基)-3-甲基苯基)-2-甲基苯甲酰胺
7-氯-1-[2-甲基-4-[(2-甲基苯甲酰)氨基]苯甲酰基]-5-氧代-2,3,4,5-四氢-1H-1-苯并氮杂卓
N-(4-(7-氯-5-氧代-2,3,4,5-四氢-1H-苯并[B]氮杂卓-1-羰基)-3-甲基苯基)-2-甲基苯甲酰胺
N-[4-[(7-氯-2,3,4,5-四氢-5-氧代-1H-1-苯并氮杂卓-1-基)羰基]-3-甲基苯基]-2-甲基苯甲酰胺
N-[4-[(7-氯-2,3,4,5-四氢-5-氧代-1H-1-苯并氮杂卓-1-基)羰基]-3-甲基苯基]-2-甲基苯甲酰胺
N-[4-[(7-CHLORO-2,3,4,5-TETRAHYDRO-5-OXO-1H-1-BENZAZEPIN-1-YL)CARBONYL]-3-METHYLPHENYL]-2-METHYLBENZAMIDE CAS号:137973-76-3
N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-oxo-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide CAS号: 137973-76-3
5-Dehydro Tolvaptan
Tolvaptan Intermediate
Tolvaptan 5-Oxo Analog
Tolvaptan impurity 5 (DM-21826)
7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-ox...
N-(4-(7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methy
N-[4-(7-chloro-5-oxo-3,4-dihydro-2H-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide
N-(4-(7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbe
7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine
物理化学性质
制备方法
933-88-0
137977-97-0
137973-76-3
向3 L反应釜中加入1-(4-氨基-2-甲基苯甲酰基)-7-氯-3,4-二氢-1H-苯并[b]氮杂卓-5(2H)-酮（70.0 g，212.90 mmol）、二氯甲烷（560 mL）和蒸馏水（140 mL），搅拌反应混合物1小时。在温度控制在10℃以下的条件下，向反应混合物中缓慢加入氢氧化镁（14.90 g，14.90 mmol），继续搅拌30分钟。随后，缓慢滴加邻甲基苯甲酰氯（30.42 mL），滴加完毕后继续搅拌反应3小时。反应完成后，过滤除去氢氧化镁，用氢氧化钠水溶液调节滤液的pH至8-9，分离有机层。有机层用无水硫酸钠干燥，过滤后减压浓缩，得到7-氯-1-[2-甲基-4-[(2-甲基苯甲酰)氨基]苯甲酰基]-5-氧代-2,3,4,5-四氢-1H-1-苯并氮杂卓91.35 g，产率为96%。
参考文献：
[1] Patent: JP2018/12690, 2018, A. Location in patent: Paragraph 0029; 0030
[2] Patent: CN105315169, 2016, A. Location in patent: Paragraph 0170; 0224; 0225
[3] Patent: CN105753735, 2016, A. Location in patent: Paragraph 0181; 0217; 0218
[4] Patent: CN106883175, 2017, A. Location in patent: Paragraph 0017; 0018
[5] Patent: CN108503586, 2018, A. Location in patent: Paragraph 0044; 0045; 0054; 0055; 0056