N-Boc-六氢-1H-氮杂卓-4-酮合成路线 （共 17 条）
反应条件
lithium borohydride in tetrahydrofuran T=0°C; 1 h; Product distribution / selectivity;
参考文献
ELI LILLY AND COMPANY
Patent: WO2009/12125 A1, 2009 ;
Location in patent: Page/Page column 30 ;
反应条件
trifluoroacetic acid in dichloromethane T=20°C; 2 h;
参考文献
Proximagen Limited; Savory, Edward Daniel; Stewart, Allson; Cartey, Allison; Brown, Giles; Simpson, Iain; Oliver, Kathryn; Patient, Lee; Higginbottom, Michael; Cole, Andrew Graham
Patent: US2013/289020 A1, 2013 ;
Location in patent: Paragraph 0341 ;
反应条件
ammonium acetate; sodium cyanoborohydride in methanol T=20°C;
参考文献
MORPHOCHEM AKTIENGESELLSCHAFT FUeR KOMBINATORISCHE CHEMIE
Patent: WO2004/35569 A2, 2004 ;
Location in patent: Page/Page column 58-59 ;
反应条件
sulfur; triethylamine in ethanol T=-5 - 20°C; 20 h;
参考文献
BAYER HEALTHCARE AG
Patent: WO2009/33581 A1, 2009 ;
Location in patent: Page/Page column 103 ;
反应条件
1: With sodium tris(acetoxy)borohydride; acetic acid in tetrahydrofuran
T=0 - 20°C;
2: With sodium hydroxide; potassium carbonate in tetrahydrofuran; water
pH=11.5;
参考文献
AMGEN INC.
Patent: WO2007/67629 A1, 2007 ;
Location in patent: Page/Page column 65-66 ;
WO 2007/067629 A1
反应条件
1.1: tetrahydrofuran / 0.25 h / 20 - 27 °C
1.2: 0 - 27 °C
2.1: CHIRALPAK AY-H / acetonitrile; isopropyl alcohol; diethylamine / |Resolution of racemate
3.1: 10 palladium hydroxide on charcoal; ammonium formate / methanol / 1.5 h / |Reflux
View Scheme
参考文献
HEPTARES THERAPEUTICS LIMITED; CONGREVE, Miles; BROWN, Giles; CANSFIELD, Julie; TEHAN, Benjamin
Patent: WO2013/72705 A1, 2013 ;
反应条件
1: Methyltriphenylphosphonium bromide With n-butyllithium in tetrahydrofuran; hexane
T=-14°C; Inert atmosphere;
2: 1-(1,1-dimethylethoxycarbonyl)-1,2,3,5,6,7-hexahydroazepin-4-one in tetrahydrofuran; hexane
T=20°C;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Patent: US2011/269737 A1, 2011 ;
Location in patent: Page/Page column 50 ;
US 20110269737 A1
