2-[(2R)-2-羟基-3-[[4-(3-氧代-4-吗啉)苯基]氨基]丙基]-1H-异吲哚-1,3(2H)-二酮合成路线 （共 13 条）
反应条件
in ethanol; water 27 h; Heating;
参考文献
Roehrig, Susanne; Straub, Alexander; Pohlmann, Jens; Lampe, Thomas; Pernerstorfer, Josef; Schlemmer, Karl-Heinz; Reinemer, Peter; Perzborn, Elisabeth
Journal of Medicinal Chemistry, 2005 , vol. 48, # 19 p. 5900 - 5908
反应条件
in N,N-dimethyl-formamide T=20 - 100°C; 3 h;
参考文献
APOTEX PHARMACHEM INC.; BODHURI, Prabhudas; WEERATUNGA, Gamini
Patent: WO2012/51692 A1, 2012 ;
Location in patent: Page/Page column 42-43 ;
反应条件
in methanol; water 20 h; Reflux;
参考文献
FARMAK, A.S.; URBASEK, Miroslav; HRADIL, Pavel; GREPL, Martin; FIALOVA, Petra; OREMUS, Vladimir; SLEZAR, Petr
Patent: WO2012/41263 A2, 2012 ;
Location in patent: Page/Page column 10 ;
参考文献
BAYER HEALTHCARE AG
Patent: US2010/160301 A1, 2010 ;
US 20100160301 A1
反应条件
in N,N-dimethyl-formamide 5 h; Reflux;
参考文献
SYMED LABS LIMITED; MOHAN RAO, dodda; KRISHNA REDDY, pingili; ANNA REDDY, ambati; VENKAT REDDY, buthukuri
Patent: WO2012/32533 A2, 2012 ;
Location in patent: Page/Page column 16 ;
反应条件
1: sodium hydroxide / ethanol; water / 0.5 h / 38 - 45 °C / pH 10 - 13 / Industry scale 2: nitric acid; sulfuric acid / sulfolane / 2 h / -5 - 30 °C 3: hydrogen / Raney Ni / methanol / 24 h / 40 - 50 °C 4: water / ethanol / 36 h / 60 °C / Industry scale View Scheme
参考文献
CADILA HEALTHCARE LIMITED; DWIVEDI, Shriprakash, Dhar; PRASAD, Ashok; PAL, Daya, Ram; SHARMA, Mukul, Hari, Prasad; JAIN, Kuldeep, Natwarlal; PATEL, Naitik, Bharatbhai
Patent: WO2013/98833 A2, 2013 ;
反应条件
1: hydrogen / Raney Ni / methanol / 24 h / 40 - 50 °C 2: water / ethanol / 36 h / 60 °C / Industry scale View Scheme
参考文献
CADILA HEALTHCARE LIMITED; DWIVEDI, Shriprakash, Dhar; PRASAD, Ashok; PAL, Daya, Ram; SHARMA, Mukul, Hari, Prasad; JAIN, Kuldeep, Natwarlal; PATEL, Naitik, Bharatbhai
Patent: WO2013/98833 A2, 2013 ;
反应条件
1: nitric acid; sulfuric acid / sulfolane / 2 h / -5 - 30 °C 2: hydrogen / Raney Ni / methanol / 24 h / 40 - 50 °C 3: water / ethanol / 36 h / 60 °C / Industry scale View Scheme
参考文献
CADILA HEALTHCARE LIMITED; DWIVEDI, Shriprakash, Dhar; PRASAD, Ashok; PAL, Daya, Ram; SHARMA, Mukul, Hari, Prasad; JAIN, Kuldeep, Natwarlal; PATEL, Naitik, Bharatbhai
Patent: WO2013/98833 A2, 2013 ;
反应条件
1.1: sodium carbonate; N-benzyl-N,N,N-triethylammonium chloride / isopropyl alcohol / 20 - 40 °C 1.2: 5 - 10 °C 2.1: water; methanol / 20 h / Reflux View Scheme
参考文献
FARMAK, A.S.; URBASEK, Miroslav; HRADIL, Pavel; GREPL, Martin; FIALOVA, Petra; OREMUS, Vladimir; SLEZAR, Petr
Patent: WO2012/41263 A2, 2012 ;
反应条件
1: methanol / 16 h / Reflux 2: N,N-dimethyl-formamide / 5 h View Scheme
参考文献
APOTEX PHARMACHEM INC.; BODHURI, Prabhudas; WEERATUNGA, Gamini
Patent: WO2012/51692 A1, 2012 ;
