(3R,4S)-4-[4-(苄氧基)苯基]-1-(4-氟苯基)-3-[3-(4-氟苯基)-3-氧代丙基]氮杂环丁烷-2-酮合成路线 （共 32 条）
反应条件
perchloric acid; p-benozquinone; palladium diacetate in water; acetonitrile 48 h; Inert atmosphere;
参考文献
Sova, Matej; Mravljak, Janez; Kovac, Andreja; Pecar, Slavko; Casar, Zdenko; Gobec, Stanislav
Synthesis, 2010 , # 20 art. no. P07810SS, p. 3433 - 3438
反应条件
1: (4-fluoro-phenyl)-magnesium bromide With zinc(II) chloride in tetrahydrofuran T=4°C; 2: 3-((3R,4S)-1-(4-fluorophenyl)-2-oxo-4-(4-(benzyloxy)phenyl)azetidin-3-yl)propionic acid chloride With tetrakis(triphenylphosphine) palladium(0) in tetrahydrofuran T=0°C; 4.5 h;
参考文献
KRKA
Patent: EP1953140 A1, 2008 ;
Location in patent: Page/Page column 16 ;
反应条件
tetrakis(triphenylphosphine) palladium(0) in tetrahydrofuran T=10°C; 1 h; Yield given;
参考文献
Journal of Medicinal Chemistry, , vol. 41, # 6 p. 973 - 980
反应条件
sulfuric acid in water; isopropyl alcohol T=20 - 25°C; 1 h; Product distribution / selectivity;
参考文献
Kansal, Vinod Kumar; Ahmad, Suhail; Sethumadhavan, Sankaran; Mariappan, Shanmugavel
Patent: US2008/58305 A1, 2008 ;
Location in patent: Page/Page column 8; 11 ;
反应条件
water; toluene-4-sulfonic acid in acetone T=20°C; 6 h; Reflux; Product distribution / selectivity;
参考文献
Gavalda I Escude, Ana; Bosch I Llado, Jordi; Vidal I Ferran, Anton; Garcia Garcia, Eva
Patent: US2009/227786 A1, 2009 ;
Location in patent: Page/Page column 17 ;
反应条件
hydrogen; Wilkinson's catalyst in dichloromethane P=3375.34 Torr; 18 h;
参考文献
WO2010/97350 A1, ;
Page/Page column 32-33 ;
反应条件
1: With hydrogenchloride; formaldehyd in tetrahydrofuran; water T=20°C; 6 h; 2: With sodium hydrogencarbonate in tetrahydrofuran; water; ethyl acetate
参考文献
WO2012/76030 A1, ;
Page/Page column 12-13 ;
反应条件
tetrakis(triphenylphosphine) palladium(0) in tetrahydrofuran T=0 - 22°C; 1.5 h;
参考文献
US2005/96307 A1, ;
Page/Page column 23-24 ;
反应条件
1: 1-bromo-4-fluorobenzene With magnesium in tetrahydrofuran T=40 - 45°C; 1 h; Heating / reflux; 2: trans-N-methoxy-N-methyl-3(R)-3-(2-oxo-4(S)-(4-benzyloxyphenyl)-1-(4-fluorophenyl)-azetidinyl)-propanamide in tetrahydrofuran T=0 - 10°C; 0.75 - 0.833333 h; 3: With hydrogenchloride in tetrahydrofuran; water T=10 - 15°C;
参考文献
WO2007/108007 A1, ;
Page/Page column 8-9 ;
反应条件
Wilkinson's catalyst; hydrogen in dichloromethane Hydrogenation; P=3102.89 Torr; 18 h;
参考文献
Wu; Wong; Chen; Ding
Journal of Organic Chemistry, 1999 , vol. 64, # 10 p. 3714 - 3718
