(R)-5-溴-3-(1-甲基-2-吡咯烷基甲基)-1H-吲哚合成路线 （共 20 条）
反应条件
1.1: isopropyl alcohol; water / 4 h / 20 - 35 °C 2.1: potassium hydroxide / toluene; water / 0.25 h / 21 - 25 °C 2.2: 4 h / 100 °C View Scheme
参考文献
F.I.S. FABBRICA ITALIANA SINTETICI S.P.A.
Patent: US2011/166364 A1, 2011 ;
反应条件
1: acetic anhydride; (R)-5-Bromo-3-[(N-methylpyrrolidin-2-yl)methyl]-1H-indole With triethylamine in acetonitrile 4.5 h; Reflux; 2: phenylsulfonylethylene With triethylamine; palladium diacetate; tris-(o-tolyl)phosphine in acetonitrile 7.5 h; Reflux;
参考文献
KANSAL, Vinod Kumar; MISTRY, Dhirenkumar N.; PATEL, Rakesh Ravjibhai; PANDEY, Saurabh
Patent: US2009/299077 A1, 2009 ;
Location in patent: Page/Page column 8 ;
反应条件
1.1: N,N-dimethyl-formamide / 95 - 100 °C 1.2: 0 - 5 °C / pH 8 - 9 2.1: N-ethyl-N,N-diisopropylamine / palladium diacetate; tris-(o-tolyl)phosphine / N,N-dimethyl-formamide / 90 - 95 °C / Inert atmosphere 3.1: water; sodium carbonate; methanol / 2 h / 25 - 30 °C 4.1: hydrogen; methanesulfonic acid / 5 palladium on charcoal / acetone / 20 °C / 2585.81 Torr 4.2: 0.5 h / 25 - 30 °C View Scheme
参考文献
Kumar, U. Sampath; Sankar, V. Ravi; Rao, M. Malleswara; Jaganathan; Buchi Reddy
Organic Process Research and Development, 2012 , vol. 16, # 12 p. 1917 - 1920
反应条件
1: triethylamine; 4-(N,N-dimethlyamino)pyridine / toluene / 0.25 h 2: tris-(o-tolyl)phosphine; triethylamine; palladium diacetate / N,N-dimethyl-formamide / 0.25 h / 25 - 120 °C 3: sodium hydrogencarbonate / methanol; water / 40 - 50 °C 4: methanesulfonic acid; 5 palladium on charcoal; hydrogen / water; acetone / 25 - 30 °C View Scheme
参考文献
Kumar, U. Sampath; Sankar, V. Ravi; Rao, M. Malleswara; Jaganathan; Buchi Reddy
Organic Process Research and Development, 2012 , vol. 16, # 12 p. 1917 - 1920
反应条件
5 Pd/C; hydrogen in ethanol T=20°C; P=5250.53 Torr; 2 h;
参考文献
Madasu, Suri Babu; Vekariya, Nagaji Ambabhai; Hari Kiran; Gupta, Badarinadh; Islam, Aminul; Douglas, Paul S.; Babu, Korupolu Raghu
Beilstein Journal of Organic Chemistry, 2012 , vol. 8, p. 1400 - 1405
反应条件
1.1: isopropyl alcohol; water / 4 h / 20 - 35 °C 2.1: potassium hydroxide / toluene; water / 0.25 h / 21 - 25 °C 2.2: 4 h / 100 °C 3.1: triethylamine / palladium diacetate; tris-(o-tolyl)phosphine / N,N-dimethyl-formamide / 5 h / 115 °C 4.1: potassium carbonate; water / methanol 5.1: hydrogen bromide / water / pH 1.5 6.1: hydrogen / 5 Pd(II)/C(eggshell) / water / 20 - 50 °C / Autoclave View Scheme
参考文献
IND-SWIFT LABORATORIES LIMITED; BHIRUD, Shekhar, Bhaskar; JOHAR, Perminder, Singh; SHARMA, Ekta; PRAJAPATY, Ramkaran; GUPTA, Chandan, Kumar
Patent: WO2012/4811 A1, 2012 ;
反应条件
1.1: triethylamine / palladium diacetate; tris-(o-tolyl)phosphine / acetonitrile / 75 - 80 °C 2.1: hydrogen / palladium 10 on activated carbon / methanol / 40 °C / 3677.86 Torr 2.2: 5 h / 25 - 70 °C View Scheme
参考文献
USV Limited B.S.D. Mar
Patent: US2012/71669 A1, 2012 ;
反应条件
N-ethyl-N,N-diisopropylamine; palladium diacetate; tris-(o-tolyl)phosphine in N,N-dimethyl-formamide T=95 - 100°C; Inert atmosphere;
参考文献
KANSAL, Vinod Kumar; MISTRY, Dhirenkumar N.; PATEL, Rakesh Ravjibhai; PANDEY, Saurabh
Patent: US2009/299077 A1, 2009 ;
Location in patent: Page/Page column 10 ;
反应条件
1.1: N,N-dimethyl-formamide / 95 - 100 °C 1.2: 0 - 5 °C / pH 8 - 9 2.1: N-ethyl-N,N-diisopropylamine / palladium diacetate; tris-(o-tolyl)phosphine / N,N-dimethyl-formamide / 90 - 95 °C / Inert atmosphere 3.1: water; sodium carbonate; methanol / 2 h / 25 - 30 °C View Scheme
参考文献
Madasu, Suri Babu; Vekariya, Nagaji Ambabhai; Hari Kiran; Gupta, Badarinadh; Islam, Aminul; Douglas, Paul S.; Babu, Korupolu Raghu
Beilstein Journal of Organic Chemistry, 2012 , vol. 8, p. 1400 - 1405
反应条件
1: triethylamine; 4-(N,N-dimethlyamino)pyridine / toluene / 0.25 h 2: tris-(o-tolyl)phosphine; triethylamine; palladium diacetate / N,N-dimethyl-formamide / 0.25 h / 25 - 120 °C 3: sodium hydroxide; methanol / 60 - 65 °C View Scheme
参考文献
Kumar, U. Sampath; Sankar, V. Ravi; Rao, M. Malleswara; Jaganathan; Buchi Reddy
Organic Process Research and Development, 2012 , vol. 16, # 12 p. 1917 - 1920
