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乙二醇
甲醛
63148-62-9
MDI
丁酮
二甲基亚砜
碳酸氢钠
471-34-1
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乙二醇
甲醛
63148-62-9
MDI
丁酮
二甲基亚砜
碳酸氢钠
471-34-1
依他普仑
合成路线
（共 38 条）
41963-20-6
4-溴-3-甲基苯甲腈
→
反应条件
128196-01-0
依他普仑
反应条件
1.1: N-bromosuccinmide; 1,1'-azobis (cyclohexanecarbonitrile) / α,α,α-trifluorotoluene / 18 h / Inert atmosphere; Reflux 2.1: N,N-dimethyl-formamide / 18 h / 90 °C / Inert atmosphere 3.1: water; sodium hydroxide / methanol / 4 h 4.1: toluene-4-sulfonic acid / dichloromethane / 15 h / 20 °C / Inert atmosphere 5.1: n-butyllithium / tetrahydrofuran / 0.17 h / -98 °C / Inert atmosphere 5.2: 1.67 h / -98 - 20 °C / Inert atmosphere 6.1: water / tetrahydrofuran / 1 h / 20 °C 7.1: magnesium sulfate / dichloromethane / 15 h / 20 °C / Inert atmosphere 8.1: N,N,N',N,-tetramethylethylenediamine; sec.-butyllithium / diethyl ether / -78 °C / Inert atmosphere 8.2: -98 - -78 °C / Inert atmosphere 9.1: toluene-4-sulfonic acid / diethyl ether / Inert atmosphere; Reflux 10.1: water; sodium tris(acetoxy)borohydride; acetic acid / dichloromethane / 16 h / 20 °C View Scheme
参考文献
Tetrahedron, , vol. 67, # 52 p. 10082 - 10088
190197-86-5
4-溴-3-(溴甲基)苯甲腈
→
反应条件
128196-01-0
依他普仑
反应条件
1.1: N,N-dimethyl-formamide / 18 h / 90 °C / Inert atmosphere 2.1: water; sodium hydroxide / methanol / 4 h 3.1: toluene-4-sulfonic acid / dichloromethane / 15 h / 20 °C / Inert atmosphere 4.1: n-butyllithium / tetrahydrofuran / 0.17 h / -98 °C / Inert atmosphere 4.2: 1.67 h / -98 - 20 °C / Inert atmosphere 5.1: water / tetrahydrofuran / 1 h / 20 °C 6.1: magnesium sulfate / dichloromethane / 15 h / 20 °C / Inert atmosphere 7.1: N,N,N',N,-tetramethylethylenediamine; sec.-butyllithium / diethyl ether / -78 °C / Inert atmosphere 7.2: -98 - -78 °C / Inert atmosphere 8.1: toluene-4-sulfonic acid / diethyl ether / Inert atmosphere; Reflux 9.1: water; sodium tris(acetoxy)borohydride; acetic acid / dichloromethane / 16 h / 20 °C View Scheme
参考文献
Tetrahedron, , vol. 67, # 52 p. 10082 - 10088
128196-01-0
依他普仑
→
反应条件
817203-55-7
+
144025-14-9
1-(4-氟苯基)-1-[3-(甲基氨基)丙基]-1,3-二氢-2-苯并呋喃-5-甲腈
反应条件
1: With β,β,β-trichloroethoxycarbonylchloride in toluene 2 h; Heating; 2: With potassium dihydrogenphosphate; zinc in tetrahydrofuran 2 h; Heating;
参考文献
Journal of Labelled Compounds and Radiopharmaceuticals, , vol. 47, # 6 p. 335 - 348
128196-01-0
依他普仑
→
反应条件
反应条件
cDNA-expressed human CYP2C19 enzyme in phosphate buffer T=37°C; pH=7.4; 1 h; Enzyme kinetics; Further Variations:Reagentssubstrate concentration;
参考文献
Olesen, Ole V.; Linnet, Kristian
Pharmacology, 1999 , vol. 59, # 6 p. 298 - 309
128196-01-0
依他普仑
→
反应条件
144025-14-9
1-(4-氟苯基)-1-[3-(甲基氨基)丙基]-1,3-二氢-2-苯并呋喃-5-甲腈
反应条件
1.1: 5 h / |Reflux 2.1: methanol / |Reflux 2.2: 20 °C View Scheme
参考文献
AARHUS UNIVERSITET; REGION MIDTJYLLAND; JENSEN, Henrik Helligsø; JENSEN, Marie; PETERSEN, Annette L.; SINNING, Steffen; WIBORG, Ove Kjær; NIELSEN, Maja Holch; BOUZINOVA, Elena; OMER, Sahar
Patent: WO2013/26455 A1, 2013 ;
144-62-7
草酸
+
128196-01-0
依他普仑
→
反应条件
219861-08-2
草酸右旋西酞普兰
反应条件
in acetone T=25 - 30°C; Industry scale;
参考文献
CIPLA LIMITED
Patent: US2010/204493 A1, 2010 ;
Location in patent: Page/Page column 8 ;
128196-01-0
依他普仑
→
反应条件
219861-08-2
草酸右旋西酞普兰
反应条件
oxalic acid in acetone T=10°C; 1 h;
参考文献
Synthon B.V.
Patent: EP1988086 A1, 2008 ;
Location in patent: Page/Page column 6 ;
128196-01-0
依他普仑
→
反应条件
766508-94-5
(S)-二去甲基氨基西酞普兰羧酸
反应条件
1.1: 2,2,2-trichloroethyl chloroformate / toluene / 2 h / Heating 1.2: 11 percent / aq. KH2PO4; Zn / tetrahydrofuran / 2 h / Heating 2.1: sodium iodide / acetone / Heating 3.1: dimethyl sulfoxide; sodium hydrogen carbonate / 0.33 h / 120 °C 4.1: 36 percent / aq. silver nitrate; aq. sodium hydroxide / ethanol / 0.5 h / 0 °C View Scheme
参考文献
Madsen, Jacob; Elfving, Betina; Andersen, Kim; Martiny, Lars; Knudsen, Gitte M.
Journal of Labelled Compounds and Radiopharmaceuticals, 2004 , vol. 47, # 6 p. 335 - 348
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