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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
220352-36-3
合成路线
(共 12 条)
1006376-61-9
(1R,2R)-2-(3,4-二氟苯基)环丙烷羧酸乙酯
→
反应条件
220352-36-3
反应条件
1: With methanol; sodium hydroxide; water in toluene T=65°C; 2 h; 2: With hydrogenchloride in water; toluene
参考文献
ASTRAZENECA AB
Patent: WO2008/18823 A1, 2008 ;
Location in patent: Page/Page column 30-31 ;
WO 2008/018823 A1
34036-07-2
3,4-二氟苯甲醛
→
反应条件
220352-36-3
反应条件
1.1: 1,8-diazabicyclo[5.4.0]undec-7-ene / toluene / 0.5 h / 40 - 45 °C 1.2: 6 h / Reflux 2.1: 2,6-bis[(4S)-isopropyl-2-oxazolin-2-yl]pyridine; dichloro(p-cymene)ruthenium(II) dimer / toluene / 50 - 55 °C 3.1: sodium hydroxide; water / methanol / 2 h / 60 - 65 °C 3.2: pH < 1.5 View Scheme
参考文献
ACTAVIS GROUP PTC EHF; Khile, Anil Shahaji; Nair, Vignesh; Trivedi, Nikhil; Pradhan, Nitin Sharadchandra
Patent: US2013/165696 A1, 2013 ;
405-03-8
3,4-二氟苯乙烯
→
反应条件
220352-36-3
反应条件
1.1: 2,6-bis[(4S)-isopropyl-2-oxazolin-2-yl]pyridine; dichloro(p-cymene)ruthenium(II) dimer / toluene / 50 - 55 °C 2.1: sodium hydroxide; water / methanol / 2 h / 60 - 65 °C 2.2: pH < 1.5 View Scheme
参考文献
ACTAVIS GROUP PTC EHF; Khile, Anil Shahaji; Nair, Vignesh; Trivedi, Nikhil; Pradhan, Nitin Sharadchandra
Patent: US2013/165696 A1, 2013 ;
112897-97-9
3,4-二氟肉桂酸
→
反应条件
220352-36-3
反应条件
1: N,N-dimethyl-formamide; oxalyl dichloride / dichloromethane / 2 h / 0 - 20 °C 2: triethylamine / dichloromethane / 3 h / 0 - 20 °C 3: palladium diacetate / dichloromethane; diethyl ether / 1 h / 0 - 20 °C 4: lithium hydroxide hydrate / tetrahydrofuran / 0.5 h / 50 °C View Scheme
参考文献
AUSPEX PHARMACEUTICALS, INC.; RAO, Tadimeti; ZHANG, Chengzhi
Patent: WO2011/17108 A2, 2011 ;
WO 2011/017108 A2
1043546-64-0
→
反应条件
220352-36-3
反应条件
1: triethylamine / dichloromethane / 3 h / 0 - 20 °C 2: palladium diacetate / dichloromethane; diethyl ether / 1 h / 0 - 20 °C 3: lithium hydroxide hydrate / tetrahydrofuran / 0.5 h / 50 °C View Scheme
参考文献
AUSPEX PHARMACEUTICALS, INC.; RAO, Tadimeti; ZHANG, Chengzhi
Patent: WO2011/17108 A2, 2011 ;
WO 2011/017108 A2
1006376-60-8
(1S)-2-氯-1-(3,4-二氟苯基)乙醇
→
反应条件
220352-36-3
反应条件
1: sodium hydroxide / water; toluene / 1 h / 40 °C 2: sodium t-butanolate / toluene / 11 h / 60 - 80 °C 3: water; sodium hydroxide / methanol / 1 h / 65 °C View Scheme
参考文献
Zhang, Hao; Liu, Jun; Zhang, Luyong; Kong, Lingyi; Yao, Hequan; Sun, Hongbin
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3598 - 3602
1006376-63-1
→
反应条件
220352-36-3
反应条件
1: sodium t-butanolate / toluene / 11 h / 60 - 80 °C 2: water; sodium hydroxide / methanol / 1 h / 65 °C View Scheme
参考文献
Zhang, Hao; Liu, Jun; Zhang, Luyong; Kong, Lingyi; Yao, Hequan; Sun, Hongbin
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3598 - 3602
367-11-3
1,2-二氟苯
→
反应条件
220352-36-3
反应条件
1: AlCl3, aluminium chloride / 1.33 h / 50 °C 2: boric acid trimethyl ester; (S)-(-)-α,α-diphenyl-2-pyrrolidinemethanol; dimethylsulfide borane complex / tetrahydrofuran; toluene / 1.5 h / 35 - 45 °C 3: sodium hydroxide / water; toluene / 1 h / 40 °C 4: sodium t-butanolate / toluene / 11 h / 60 - 80 °C 5: water; sodium hydroxide / methanol / 1 h / 65 °C View Scheme
参考文献
Zhang, Hao; Liu, Jun; Zhang, Luyong; Kong, Lingyi; Yao, Hequan; Sun, Hongbin
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3598 - 3602
51336-95-9
2-氯-1-(3,4-二氟苯基)乙酮
→
反应条件
220352-36-3
反应条件
1: boric acid trimethyl ester; (S)-(-)-α,α-diphenyl-2-pyrrolidinemethanol; dimethylsulfide borane complex / tetrahydrofuran; toluene / 1.5 h / 35 - 45 °C 2: sodium hydroxide / water; toluene / 1 h / 40 °C 3: sodium t-butanolate / toluene / 11 h / 60 - 80 °C 4: water; sodium hydroxide / methanol / 1 h / 65 °C View Scheme
参考文献
Zhang, Hao; Liu, Jun; Zhang, Luyong; Kong, Lingyi; Yao, Hequan; Sun, Hongbin
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3598 - 3602
220352-36-3
→
反应条件
274693-27-5
替格瑞洛
反应条件
1.1: triethylamine; diphenyl phosphoryl azide / toluene / 1 h / Reflux 1.2: 16 h / Reflux 2.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 16 h / 20 °C 3.1: hydrogenchloride / water; methanol / 3 h / 20 °C 3.2: pH 8 - 9 View Scheme
参考文献
WO2011/17108 A2, ;
WO 2011/017108 A2
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