2-[2-[3(S)-[3-(7-氯-2-喹啉基)乙烯基]苯基]-3-羟基丙基]苯基-2-丙醇合成路线 (共 18 条)
反应条件
1: methyl-magnesium chloride With cerium(III) chloride in tetrahydrofuran T=-5 - 0°C; 2.5 h; 2: lt;S-(E)gt;-2-lt;3-lt;3-lt;2-(7-chloro-2-quinolinyl)ethenylgt;phenylgt;-3-hydroxypropylgt;benzoic acid methyl ester in tetrahydrofuran; toluene T=3 - 5°C; 2.25 h; 3: With water; sodium carbonate; acetic acid more than 3 stages;
参考文献
PLIVA ISTRAZIVANJE I RAZVOJ D.O.O.; MCLEISH, Nicholas, Alistair, Maxwell
Patent: WO2008/9970 A2, 2008 ;
Location in patent: Page/Page column 25 ;
反应条件
1: lt;S-(E)gt;-2-lt;3-lt;3-lt;2-(7-chloro-2-quinolinyl)ethenylgt;phenylgt;-3-hydroxypropylgt;benzoic acid methyl ester With Lanthanum chloride; lithium chloride in tetrahydrofuran T=20°C; 1 h; 2: methyl-magnesium chloride in tetrahydrofuran T=-5 - 0°C; 12 h; 3: With water; ammonium chloride in tetrahydrofuran T=20 - 25°C; Product distribution / selectivity;
参考文献
Lonza AG
Patent: EP2014633 A1, 2009 ;
Location in patent: Page/Page column 4-5 ;
反应条件
triethylamine; tris-(o-tolyl)phosphine; palladium diacetate in N,N-dimethyl-formamide T=100°C; Heck reaction; 3 h;
参考文献
Caspi, Daniel D.; Ebner, David C.; Bagdanoff, Jeffrey T.; Stoltz, Brian M.
Advanced Synthesis and Catalysis, 2004 , vol. 346, # 2-3 p. 185 - 189
反应条件
1: With Lanthanum chloride; lithium chloride in tetrahydrofuran T=5 - 20°C; 1 h; 2: With water; acetic acid in tetrahydrofuran; tert-butyl methyl ether T=10°C;
参考文献
Lonza AG
Patent: EP2014650 A1, 2009 ;
Location in patent: Page/Page column 4 ;
反应条件
cerium(III) chloride in tetrahydrofuran; toluene T=0°C; Grignard addition; 2 h; Product distribution; Further Variations:Reaction partnerscatalyst crystal habit;
参考文献
Sunil Kumar; Anjaneyulu; Hima Bindu
Asian Journal of Chemistry, 2011 , vol. 23, # 10 p. 4536 - 4546
反应条件
1: 91 percent / NaBH4 / ethanol / 3.5 h / 0 - 23 °C 2: 93 percent / tetrahydrofuran; diethyl ether / 3.5 h / 23 °C 3: (-)-sparteine; O2; Cs2CO3 / Pd(nbd)Cl2 / toluene; 2-methyl-propan-2-ol / 4.5 h / 80 °C / 760.05 Torr 4: 90 percent / P(o-tolyl)3; Et3N / Pd(OAc)2 / dimethylformamide / 3 h / 100 °C View Scheme
参考文献
Caspi, Daniel D.; Ebner, David C.; Bagdanoff, Jeffrey T.; Stoltz, Brian M.
Advanced Synthesis and Catalysis, 2004 , vol. 346, # 2-3 p. 185 - 189
反应条件
1: 93 percent / tetrahydrofuran; diethyl ether / 3.5 h / 23 °C 2: (-)-sparteine; O2; Cs2CO3 / Pd(nbd)Cl2 / toluene; 2-methyl-propan-2-ol / 4.5 h / 80 °C / 760.05 Torr 3: 90 percent / P(o-tolyl)3; Et3N / Pd(OAc)2 / dimethylformamide / 3 h / 100 °C View Scheme
参考文献
Caspi, Daniel D.; Ebner, David C.; Bagdanoff, Jeffrey T.; Stoltz, Brian M.
Advanced Synthesis and Catalysis, 2004 , vol. 346, # 2-3 p. 185 - 189
反应条件
1: (-)-sparteine; O2; Cs2CO3 / Pd(nbd)Cl2 / toluene; 2-methyl-propan-2-ol / 4.5 h / 80 °C / 760.05 Torr 2: 90 percent / P(o-tolyl)3; Et3N / Pd(OAc)2 / dimethylformamide / 3 h / 100 °C View Scheme
参考文献
Caspi, Daniel D.; Ebner, David C.; Bagdanoff, Jeffrey T.; Stoltz, Brian M.
Advanced Synthesis and Catalysis, 2004 , vol. 346, # 2-3 p. 185 - 189
反应条件
1: NaBH4 / ethanol / 0 - 23 °C 2: (-)-sparteine; O2; Cs2CO3 / Pd(nbd)Cl2 / toluene; 2-methyl-propan-2-ol / 4.5 h / 80 °C / 760.05 Torr 3: 90 percent / P(o-tolyl)3; Et3N / Pd(OAc)2 / dimethylformamide / 3 h / 100 °C View Scheme
参考文献
Caspi, Daniel D.; Ebner, David C.; Bagdanoff, Jeffrey T.; Stoltz, Brian M.
Advanced Synthesis and Catalysis, 2004 , vol. 346, # 2-3 p. 185 - 189
反应条件
1: With sodium hydroxide; ethanol; water 30 h; Heating / reflux; 2: With hydrogenchloride; water in toluene pH=5.6; 0.5 h; Product distribution / selectivity;
参考文献
ESTEVE QUIMICA, S.A.
Patent: EP1886997 A1, 2008 ;
Location in patent: Page/Page column 7 ;