2-氯-1-(3,4-二氟苯基)乙酮合成路线 （共 8 条）
反应条件
1: chloroacetyl chloride With AlCl3, aluminium chloride in dichloromethane 0.166667 h; Heating / reflux; 2: ortho-difluorobenzene in dichloromethane 3 h; Heating / reflux;
参考文献
sanofi-aventis
Patent: US7038044 B1, 2006 ;
Location in patent: Page/Page column 26-27 ;
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
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 5: thionyl chloride / 8 h / 35 °C 6: ammonia; water / ethyl acetate / 1 h / 10 °C 7: sodium hypochlorite; water; sodium hydroxide / 14 h / 40 °C 8: N-ethyl-N,N-diisopropylamine / dichloromethane / 16 h 9: hydrogenchloride; water / methanol / 1 h View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 22, # 11 p. 3598 - 3602
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 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
反应条件
boric acid trimethyl ester; (S)-(-)-α,α-diphenyl-2-pyrrolidinemethanol; dimethylsulfide borane complex in tetrahydrofuran; toluene T=35 - 45°C; 1.5 h; optical yield given as percent ee;
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
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 5: thionyl chloride / 8 h / 35 °C 6: ammonia; water / ethyl acetate / 1 h / 10 °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
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 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
参考文献
Yamane, Noriko; Tanaka, Yoshikazu; Ohyabu, Naoki; Yamane, Shoji; Maekawa, Kazuhiko; Ishizaki, Jun; Suzuki, Ryuji; Itoh, Tsunetoshi; Takemoto, Hiroshi
European Journal of Pharmacology, 2008 , vol. 586, # 1-3 p. 44 - 51
