N-[3-[3-[3-[4-(3-氨基丙基氨基)丁基氨基]丙基氨基]丙基-羟基氨基]丙基]-2-(1H-吲哚-3-基)乙酰胺合成路线 (共 28 条)
反应条件
1.1: 98 percent / Et3N; DMAP / CH2Cl2 / 1 h / 20 °C 2.1: 97 percent / Cs2CO3; thiophenol / acetonitrile / 10 h / 20 °C 3.1: 93 percent / ethanol / 24 h / 60 °C 4.1: 98 percent / ammonium fluoride / acetonitrile / 10 h / 60 °C 5.1: 90 percent / Ph3P; DEAD / CH2Cl2; benzene; toluene / 0.17 h / 20 °C 6.1: m-CPBA / CH2Cl2 / 1 h / -10 °C 6.2: 90 percent / Me2S / CH2Cl2 / -10 - 20 °C 7.1: 95 percent / SOCl2 / CH2Cl2; methanol / 2.5 h / 20 °C 8.1: 4(chlorodiphenylmethyl)phenoxymethylated polystyrene polymer; iPr2NEt / CH2Cl2 / 24 h / 20 °C 8.2: 2-mercaptoethanol; DBU / dimethylformamide / 26 h / 20 °C 8.3: TFA / CH2Cl2 / 0.08 h / 20 °C View Scheme
参考文献
Hidai; Kan; Fukuyama
Chemical and Pharmaceutical Bulletin, 2000 , vol. 48, # 10 p. 1570 - 1576
反应条件
1.1: 98 percent / ammonium fluoride / acetonitrile / 10 h / 60 °C 2.1: 90 percent / Ph3P; DEAD / CH2Cl2; benzene; toluene / 0.17 h / 20 °C 3.1: m-CPBA / CH2Cl2 / 1 h / -10 °C 3.2: 90 percent / Me2S / CH2Cl2 / -10 - 20 °C 4.1: 95 percent / SOCl2 / CH2Cl2; methanol / 2.5 h / 20 °C 5.1: 4(chlorodiphenylmethyl)phenoxymethylated polystyrene polymer; iPr2NEt / CH2Cl2 / 24 h / 20 °C 5.2: 2-mercaptoethanol; DBU / dimethylformamide / 26 h / 20 °C 5.3: TFA / CH2Cl2 / 0.08 h / 20 °C View Scheme
参考文献
Hidai; Kan; Fukuyama
Chemical and Pharmaceutical Bulletin, 2000 , vol. 48, # 10 p. 1570 - 1576
反应条件
1.1: 94 percent / Et3N / CH2Cl2 / 0.5 h / 20 °C 2.1: 90 percent / Ph3P; DEAD / CH2Cl2; benzene; toluene / 0.17 h / 20 °C 3.1: m-CPBA / CH2Cl2 / 1 h / -10 °C 3.2: 90 percent / Me2S / CH2Cl2 / -10 - 20 °C 4.1: 95 percent / SOCl2 / CH2Cl2; methanol / 2.5 h / 20 °C 5.1: 4(chlorodiphenylmethyl)phenoxymethylated polystyrene polymer; iPr2NEt / CH2Cl2 / 24 h / 20 °C 5.2: 2-mercaptoethanol; DBU / dimethylformamide / 26 h / 20 °C 5.3: TFA / CH2Cl2 / 0.08 h / 20 °C View Scheme
参考文献
Hidai; Kan; Fukuyama
Chemical and Pharmaceutical Bulletin, 2000 , vol. 48, # 10 p. 1570 - 1576
反应条件
1.1: 97 percent / Cs2CO3; thiophenol / acetonitrile / 10 h / 20 °C 2.1: 93 percent / ethanol / 24 h / 60 °C 3.1: 98 percent / ammonium fluoride / acetonitrile / 10 h / 60 °C 4.1: 90 percent / Ph3P; DEAD / CH2Cl2; benzene; toluene / 0.17 h / 20 °C 5.1: m-CPBA / CH2Cl2 / 1 h / -10 °C 5.2: 90 percent / Me2S / CH2Cl2 / -10 - 20 °C 6.1: 95 percent / SOCl2 / CH2Cl2; methanol / 2.5 h / 20 °C 7.1: 4(chlorodiphenylmethyl)phenoxymethylated polystyrene polymer; iPr2NEt / CH2Cl2 / 24 h / 20 °C 7.2: 2-mercaptoethanol; DBU / dimethylformamide / 26 h / 20 °C 7.3: TFA / CH2Cl2 / 0.08 h / 20 °C View Scheme
参考文献
Hidai; Kan; Fukuyama
Chemical and Pharmaceutical Bulletin, 2000 , vol. 48, # 10 p. 1570 - 1576
反应条件
1.1: 99 percent / Ph3P; Pd(PPh3)4; pyrrolidine / CH2Cl2 / 1.5 h / 20 °C 2.1: 94 percent / Et3N / CH2Cl2 / 0.5 h / 20 °C 3.1: 90 percent / Ph3P; DEAD / CH2Cl2; benzene; toluene / 0.17 h / 20 °C 4.1: m-CPBA / CH2Cl2 / 1 h / -10 °C 4.2: 90 percent / Me2S / CH2Cl2 / -10 - 20 °C 5.1: 95 percent / SOCl2 / CH2Cl2; methanol / 2.5 h / 20 °C 6.1: 4(chlorodiphenylmethyl)phenoxymethylated polystyrene polymer; iPr2NEt / CH2Cl2 / 24 h / 20 °C 6.2: 2-mercaptoethanol; DBU / dimethylformamide / 26 h / 20 °C 6.3: TFA / CH2Cl2 / 0.08 h / 20 °C View Scheme
参考文献
Hidai; Kan; Fukuyama
Chemical and Pharmaceutical Bulletin, 2000 , vol. 48, # 10 p. 1570 - 1576
反应条件
1.1: 90 percent / Ph3P; DEAD / CH2Cl2; benzene; toluene / 0.17 h / 20 °C 2.1: m-CPBA / CH2Cl2 / 1 h / -10 °C 2.2: 90 percent / Me2S / CH2Cl2 / -10 - 20 °C 3.1: 95 percent / SOCl2 / CH2Cl2; methanol / 2.5 h / 20 °C 4.1: 4(chlorodiphenylmethyl)phenoxymethylated polystyrene polymer; iPr2NEt / CH2Cl2 / 24 h / 20 °C 4.2: 2-mercaptoethanol; DBU / dimethylformamide / 26 h / 20 °C 4.3: TFA / CH2Cl2 / 0.08 h / 20 °C View Scheme
参考文献
Hidai; Kan; Fukuyama
Chemical and Pharmaceutical Bulletin, 2000 , vol. 48, # 10 p. 1570 - 1576
反应条件
1.1: 95 percent / SOCl2 / CH2Cl2; methanol / 2.5 h / 20 °C 2.1: 4(chlorodiphenylmethyl)phenoxymethylated polystyrene polymer; iPr2NEt / CH2Cl2 / 24 h / 20 °C 2.2: 2-mercaptoethanol; DBU / dimethylformamide / 26 h / 20 °C 2.3: TFA / CH2Cl2 / 0.08 h / 20 °C View Scheme
参考文献
Hidai; Kan; Fukuyama
Chemical and Pharmaceutical Bulletin, 2000 , vol. 48, # 10 p. 1570 - 1576
反应条件
1.1: m-CPBA / CH2Cl2 / 1 h / -10 °C 1.2: 90 percent / Me2S / CH2Cl2 / -10 - 20 °C 2.1: 95 percent / SOCl2 / CH2Cl2; methanol / 2.5 h / 20 °C 3.1: 4(chlorodiphenylmethyl)phenoxymethylated polystyrene polymer; iPr2NEt / CH2Cl2 / 24 h / 20 °C 3.2: 2-mercaptoethanol; DBU / dimethylformamide / 26 h / 20 °C 3.3: TFA / CH2Cl2 / 0.08 h / 20 °C View Scheme
参考文献
Hidai; Kan; Fukuyama
Chemical and Pharmaceutical Bulletin, 2000 , vol. 48, # 10 p. 1570 - 1576