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结构式
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
萘福昔定
合成路线
(共 10 条)
1729-38-0
4-(6-甲氧基-2-苯基-3,4-二氢萘并醛烯-1-基)苯酚
+
7250-67-1
N-(2-氯乙基)吡咯烷盐酸盐
→
反应条件
1845-11-0
萘福昔定
反应条件
1: 1-(p-hydroxyphenyl)-6-methoxy-2-phenyl-3,4-dihydronaphthalene With sodium hydride in N,N-dimethyl-formamide T=20°C; 0.333333 h; 2: N-(2-chloroethyl)-pyrrolidine hydrochloride in N,N-dimethyl-formamide T=50°C; 11 h;
参考文献
Nakata, Kenya; Sano, Yoshiyuki; Shiina, Isamu
Molecules, 2010 , vol. 15, # 10 p. 6773 - 6794
1081-73-8
1-(2-(4-溴苯氧基)乙基)吡咯烷
+
1769-84-2
6-甲氧基-2-苯基四氢萘酮
→
反应条件
1845-11-0
萘福昔定
反应条件
1: 1-[2-(4-bromo-phenoxy)-ethyl]-pyrrolidine With n-butyllithium; cerium(III) chloride in tetrahydrofuran; hexane T=-78°C; 4 h; 2: (6-methoxy-2-phenyl-3,4-dihydronaphthalene-1(2H)-one) in tetrahydrofuran; hexane T=20°C; 16 h;
参考文献
LEK PHARMACEUTICALS D.D.; GAZIC SMILOVIC, Ivana; SEECHURN, Carin; COLACOT, Thomas J.
Patent: WO2012/159981 A2, 2012 ;
Location in patent: Page/Page column 20-21 ;
180915-95-1
1-{2-[4-(2-溴-6-甲氧基-3,4-二氢-1-萘基)苯氧基]乙基}吡咯烷
+
98-80-6
苯硼酸
→
反应条件
1845-11-0
萘福昔定
反应条件
sodium carbonate; tetrakis(triphenylphosphine) palladium(0) in tetrahydrofuran; water 18 h; Reflux;
参考文献
GLENMARK GENERICS LIMITED; KHAN, Mubeen Ahmed; TRIVEDI, Nikhil Rasiklal; KANDASAMY, Nagan Nirmalan; PATIL, Dayaghan Gangadhar; PANDEY, Vipin Kumar; SINHA, Sukumar
Patent: WO2010/125578 A2, 2010 ;
Location in patent: Page/Page column 20; 21 ;
5050-41-9
N-(2-氯乙基)吡咯烷
+
1729-38-0
4-(6-甲氧基-2-苯基-3,4-二氢萘并醛烯-1-基)苯酚
→
反应条件
1845-11-0
萘福昔定
反应条件
sodium hydride in N,N-dimethyl-formamide T=50°C;
参考文献
Sano, Yoshiyuki; Nakata, Kenya; Otoyama, Takafumi; Umeda, Sei; Shiina, Isamu
Chemistry Letters, 2007 , vol. 36, # 1 p. 40 - 41
123-75-1
四氢吡咯
+
1449689-98-8
→
反应条件
1845-11-0
萘福昔定
反应条件
in ethanol T=100°C; 4 h; Inert atmosphereSealed tube;
参考文献
Walkinshaw, Andrew J.; Xu, Wenshu; Suero, Marcos G.; Gaunt, Matthew J.
Journal of the American Chemical Society, 2013 , vol. 135, # 34 p. 12532 - 12535
1078-19-9
6-甲氧基-1-萘满酮
→
反应条件
1845-11-0
萘福昔定
反应条件
1.1: sodium t-butanolate / PdCl2(Amphos)2 / toluene / 18 h / 60 °C / Inert atmosphere 2.1: n-butyllithium; cerium(III) chloride / hexane; tetrahydrofuran / 2 h / -78 °C 2.2: 16 h / 20 °C View Scheme
参考文献
LEK PHARMACEUTICALS D.D.; GAZIC SMILOVIC, Ivana; SEECHURN, Carin; COLACOT, Thomas J.
Patent: WO2012/159981 A2, 2012 ;
17878-44-3
对(三甲基硅氧基)溴苯
→
反应条件
1845-11-0
萘福昔定
反应条件
1: 1.) Mg / 1.) THF, 2.) THF, room temp, 1 h; reflux, 1 h 2: 72 percent / K2CO3, / acetone / 15 h / Heating View Scheme
参考文献
Bindal, Rajeshwar D.; Durani, S.; Kapil, Randhir S.; Anand, Nitya
Synthesis, 1982 , # 5 p. 405 - 407
1769-84-2
6-甲氧基-2-苯基四氢萘酮
→
反应条件
1845-11-0
萘福昔定
反应条件
1: 1.) Mg / 1.) THF, 2.) THF, room temp, 1 h; reflux, 1 h 2: 72 percent / K2CO3, / acetone / 15 h / Heating View Scheme
参考文献
Bindal, Rajeshwar D.; Durani, S.; Kapil, Randhir S.; Anand, Nitya
Synthesis, 1982 , # 5 p. 405 - 407
1845-11-0
萘福昔定
→
反应条件
180916-16-9
拉索昔芬
反应条件
1: H2 / Pd(OH)2/C 2: BBr3 View Scheme
参考文献
Rosati; Jardine; Cameron; Thompson; Hua Zhu Ke; Toler; Brown; Pan; Ebbinghaus; Reinhold; Elliott; Newhouse; Tjoa; Sweetnam; Cole; Arriola; Gauthier; Crawford; Nickerson; Pirie; Qi; Simmons; Tkalcevic
Journal of Medicinal Chemistry, 1998 , vol. 41, # 16 p. 2928 - 2931
1845-11-0
萘福昔定
→
反应条件
1847-63-8
1-[2-[4-(3,4-二氢-6-甲氧基-2-苯基-1-萘基)苯氧基]乙基]吡咯烷盐酸盐
反应条件
hydrogenchloride in dichloromethane; di-isopropyl ether; ethyl acetate 2 h;
参考文献
GLENMARK GENERICS LIMITED; KHAN, Mubeen Ahmed; TRIVEDI, Nikhil Rasiklal; KANDASAMY, Nagan Nirmalan; PATIL, Dayaghan Gangadhar; PANDEY, Vipin Kumar; SINHA, Sukumar
Patent: WO2010/125578 A2, 2010 ;
Location in patent: Page/Page column 20; 21 ;