4-氨基-N-[2-(二乙基氨基)乙基]-2-甲氧基苯甲酰胺合成路线 （共 11 条）
反应条件
in acetonitrile T=20°C; Acetylation; 1 h;
参考文献
Eisenhut; Hull; Mohammed; Mier; Lay; Just; Gorgas; Lehmann; Haberkorn
Journal of Medicinal Chemistry, 2000 , vol. 43, # 21 p. 3913 - 3922
反应条件
hydrogen; palladium 10 on activated carbon in ethanol
48 h;
参考文献
7TM PHARMA A/S
Patent: WO2003/87045 A1, 2003 ;
Location in patent: Page/Page column 69-70 ;
WO 03/087045 A1
反应条件
potassium hydroxide in methanol; water
参考文献
Pham, Tien Q.; Greguric, Ivan; Liu, Xiang; Berghofer, Paula; Ballantyne, Patrice; Chapman, Janette; Mattner, Filomena; Dikic, Branko; Jackson, Timothy; Loc'h, Christian; Katsifis, Andrew
Journal of Medicinal Chemistry, 2007 , vol. 50, # 15 p. 3561 - 3572
反应条件
1: [O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium]*BF4; N,N-diisopropylethylamine / dimethylformamide / 2 h / 20 °C
2: H2 / Pd/C / methanol / 4 h / 20 °C / atmospheric pressure
View Scheme
参考文献
Lazar, Carmen; Kluczyk, Alicja; Kiyota, Taira; Konishi, Yasuo
Journal of Medicinal Chemistry, 2004 , vol. 47, # 27 p. 6973 - 6982
反应条件
1: [O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium]*BF4; N,N-diisopropylethylamine / dimethylformamide / 2 h / 20 °C
2: H2 / Pd/C / methanol / 4 h / 20 °C / atmospheric pressure
View Scheme
参考文献
Lazar, Carmen; Kluczyk, Alicja; Kiyota, Taira; Konishi, Yasuo
Journal of Medicinal Chemistry, 2004 , vol. 47, # 27 p. 6973 - 6982
反应条件
1: 89 percent / ethanol / 2 h / 50 °C
2: KOH / methanol; H2O / 2 h / Heating
3: 10.2 g / acetic acid / 2 h / 50 °C
4: thionyl chloride / tetrahydrofuran / 2 h / Heating
5: 1.2 g / triethylamine / tetrahydrofuran / 2 h
6: 74 percent / KOH / methanol; H2O
View Scheme
参考文献
Pham, Tien Q.; Greguric, Ivan; Liu, Xiang; Berghofer, Paula; Ballantyne, Patrice; Chapman, Janette; Mattner, Filomena; Dikic, Branko; Jackson, Timothy; Loc'h, Christian; Katsifis, Andrew
Journal of Medicinal Chemistry, 2007 , vol. 50, # 15 p. 3561 - 3572
反应条件
1: 10.2 g / acetic acid / 2 h / 50 °C
2: thionyl chloride / tetrahydrofuran / 2 h / Heating
3: 1.2 g / triethylamine / tetrahydrofuran / 2 h
4: 74 percent / KOH / methanol; H2O
View Scheme
参考文献
Pham, Tien Q.; Greguric, Ivan; Liu, Xiang; Berghofer, Paula; Ballantyne, Patrice; Chapman, Janette; Mattner, Filomena; Dikic, Branko; Jackson, Timothy; Loc'h, Christian; Katsifis, Andrew
Journal of Medicinal Chemistry, 2007 , vol. 50, # 15 p. 3561 - 3572
反应条件
1: thionyl chloride / tetrahydrofuran / 2 h / Heating
2: 1.2 g / triethylamine / tetrahydrofuran / 2 h
3: 74 percent / KOH / methanol; H2O
View Scheme
参考文献
Pham, Tien Q.; Greguric, Ivan; Liu, Xiang; Berghofer, Paula; Ballantyne, Patrice; Chapman, Janette; Mattner, Filomena; Dikic, Branko; Jackson, Timothy; Loc'h, Christian; Katsifis, Andrew
Journal of Medicinal Chemistry, 2007 , vol. 50, # 15 p. 3561 - 3572
反应条件
1: KOH / methanol; H2O / 2 h / Heating
2: 10.2 g / acetic acid / 2 h / 50 °C
3: thionyl chloride / tetrahydrofuran / 2 h / Heating
4: 1.2 g / triethylamine / tetrahydrofuran / 2 h
5: 74 percent / KOH / methanol; H2O
View Scheme
参考文献
Pham, Tien Q.; Greguric, Ivan; Liu, Xiang; Berghofer, Paula; Ballantyne, Patrice; Chapman, Janette; Mattner, Filomena; Dikic, Branko; Jackson, Timothy; Loc'h, Christian; Katsifis, Andrew
Journal of Medicinal Chemistry, 2007 , vol. 50, # 15 p. 3561 - 3572
反应条件
1: 12 h / 20 °C
2: H2 / ethanol / 12 h / 20 °C
View Scheme
参考文献
Receveur, Jean-Marie; Bjurling, Emelie; Ulven, Trond; Little, Paul Brian; Norregaard, Pia K.; Hoegberg, Thomas
Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 20 p. 5075 - 5080
