(1H-吲哚-3-基)(2,2,3,3-四甲基环丙基)甲酮合成路线 (共 4 条)
反应条件
1: 1H-indol-3-yl-(2,2,3,3-tetramethylcyclopropyl)methanone With sodium hydride in N,N-dimethyl-formamide; mineral oil T=0 - 20°C; 2: n-bromopentane in N,N-dimethyl-formamide; mineral oil T=0 - 45°C;
参考文献
Frost, Jennifer M.; Dart, Michael J.; Tietje, Karin R.; Garrison, Tiffany R.; Grayson, George K.; Daza, Anthony V.; El-Kouhen, Odile F.; Yao, Betty B.; Hsieh, Gin C.; Pai, Madhavi; Zhu, Chang Z.; Chandran, Prasant; Meyer, Michael D.
Journal of Medicinal Chemistry, 2010 , vol. 53, # 1 p. 295 - 315
反应条件
1: 1H-indol-3-yl-(2,2,3,3-tetramethylcyclopropyl)methanone With sodium hydride in N,N-dimethyl-formamide; mineral oil T=0 - 20°C; 2: 1-bromo-butane in N,N-dimethyl-formamide; mineral oil T=0 - 45°C;
参考文献
Frost, Jennifer M.; Dart, Michael J.; Tietje, Karin R.; Garrison, Tiffany R.; Grayson, George K.; Daza, Anthony V.; El-Kouhen, Odile F.; Yao, Betty B.; Hsieh, Gin C.; Pai, Madhavi; Zhu, Chang Z.; Chandran, Prasant; Meyer, Michael D.
Journal of Medicinal Chemistry, 2010 , vol. 53, # 1 p. 295 - 315
反应条件
1: indole With ethylmagnesium bromide in tetrahydrofuran; dichloromethane
T=20°C; 0.25 h;
2: With zinc(II) chloride in tetrahydrofuran; dichloromethane
T=20°C; 0.5 h;
3: 2,2,3,3-tetramethyl-cyclopropane-1-carboxylic acid chloride in tetrahydrofuran; dichloromethane
T=20°C; 6 h;
参考文献
ABBOTT LABORATORIES
Patent: WO2006/69196 A1, 2006 ;
Location in patent: Page/Page column 32 ;
WO 2006/069196 A1
反应条件
ethylmagnesium bromide; zinc(II) chloride
参考文献
Yao; Hsieh; Frost; Fan; Garrison; Daza; Grayson; Zhu; Pai; Chandran; Salyers; Wensink; Honore; Sullivan; Dart; Meyer
British Journal of Pharmacology, 2008 , vol. 153, # 2 p. 390 - 401