1-(1-(3-甲氧基-4-硝基苯基)哌啶-4-基)-4-甲基哌嗪合成路线 （共 6 条）
反应条件
1: 2-methoxy-4-[4-(4-methylpiperazin-1-yl)-piperidin-1-yl]-phenylamine With methanesulfonic acid in ethanol T=20°C; 0.25 h; 2: 1-[1-(3-methoxy-4-nitrophenyl)piperidin-4-yl]-4-methylpiperazine in ethanol T=100°C; 5 h;
参考文献
Astellas Pharma Inc.; OBITSU, Kazuyoshi; AKIBA, Takahiro; KOBAYASHI, Koji; HIRASAWA, Shun; KONDOH, Yutaka; TAKEGUCHI, Kazuhiro; TAKAHAMA, Yuji; ORII, Ryoki
Patent: EP2669281 A1, 2013 ;
Location in patent: Paragraph 0046 ;
反应条件
1.1: 5 palladium on charcoal; hydrogen / ethanol / 8 h / 20 °C 2.1: methanesulfonic acid / ethanol / 0.25 h / 20 °C 2.2: 5 h / 100 °C View Scheme
参考文献
Astellas Pharma Inc.; OBITSU, Kazuyoshi; AKIBA, Takahiro; KOBAYASHI, Koji; HIRASAWA, Shun; KONDOH, Yutaka; TAKEGUCHI, Kazuhiro; TAKAHAMA, Yuji; ORII, Ryoki
Patent: EP2669281 A1, 2013 ;
反应条件
potassium carbonate in dichloromethane; N,N-dimethyl-formamide
T=70°C;
参考文献
ABBOTT LABORATORIES
Patent: US2011/15172 A1, 2011 ;
Location in patent: Page/Page column 34 ;
反应条件
1: in dichloromethane
T=0 - 20°C; 4 h;
2: With sodium tris(acetoxy)borohydride
T=20°C; 24 h;
参考文献
NOVARTIS AG; NOVARTIS PHARMA GMBH
Patent: WO2004/80980 A1, 2004 ;
Location in patent: Page 132 ;
WO 2004/080980 A1
反应条件
1.1: potassium carbonate / N,N-dimethyl-formamide / 70 °C
2.1: 1,2-dichloro-ethane / 0.5 h
2.2: 20 °C
View Scheme
参考文献
Astellas Pharma Inc.; OBITSU, Kazuyoshi; AKIBA, Takahiro; KOBAYASHI, Koji; HIRASAWA, Shun; KONDOH, Yutaka; TAKEGUCHI, Kazuhiro; TAKAHAMA, Yuji; ORII, Ryoki
Patent: EP2669281 A1, 2013 ;
反应条件
1.1: potassium carbonate / N,N-dimethyl-formamide / 70 °C
2.1: 1,2-dichloro-ethane / 0.5 h
2.2: 20 °C
View Scheme
参考文献
Astellas Pharma Inc.; OBITSU, Kazuyoshi; AKIBA, Takahiro; KOBAYASHI, Koji; HIRASAWA, Shun; KONDOH, Yutaka; TAKEGUCHI, Kazuhiro; TAKAHAMA, Yuji; ORII, Ryoki
Patent: EP2669281 A1, 2013 ;
