1-Boc-氮杂环丁烷-3-羧酸合成路线 (共 19 条)
反应条件
triethylamine in methanol T=20°C; 18 h;
参考文献
AstraZeneca AB
Patent: US2008/171732 A1, 2008 ;
Location in patent: Page/Page column 36 ;
US 20080171732 A1
反应条件
triethylamine in dichloromethane T=20°C; 18 h;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; COGAN, Derek; MOSS, Neil; SARKO, Christopher Ronald; BAMFORD, Samantha Jayne; LOKE, Pui Leng; NAPIER, Spencer Charles, R.; TYE, Heather; WHITTAKER, Mark
Patent: WO2010/80357 A1, 2010 ;
Location in patent: Page/Page column 45 ;
WO 2010/080357 A1
反应条件
1: With water; sodium hydroxide in methanol 5 h; Reflux; 2: With citric acid in water
参考文献
PFIZER LIMITED; ACIRO, Caroline; BAGAL, Sharanjeet Kaur; HARVEY, John Wilson; JONES, Lyn Howard; MOWBRAY, Charles Eric; OWEN, Robert McKenzie; SABNIS, Yogesh Anil; STORER, Robert Ian; YEAP, Siew Kuen
Patent: WO2010/131145 A1, 2010 ;
Location in patent: Page/Page column 86 ;
反应条件
sodium hydroxide in tetrahydrofuran; diethyl ether; water
反应条件
1: Et3N 2: aq. NaOH View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 12, # 5 p. 757 - 761
反应条件
diazomethyl-trimethyl-silane in toluene T=0 - 20°C; 0.916667 h;
参考文献
PFIZER INC.
Patent: WO2006/21881 A2, 2006 ;
Location in patent: Page/Page column 61 ;
WO 2006/021881 A2
反应条件
in methanol; toluene T=0 - 20°C; 0.916667 h;
参考文献
AGOURON PHARMACEUTICALS, INC.
Patent: US2006/46991 A1, 2006 ;
Location in patent: Page/Page column 55-56 ;
US 20060046991 A1
反应条件
1: 2,2-Dimethyl-[1,3]dioxane-4,6-dione; 3-carboxyazetidine-1-carboxylic acid tert-butyl ester With 4-(N,N-dimethlyamino)pyridine; 1,1'-carbonyldiimidazole in dichloromethane T=0 - 20°C; 2: ethanol 6 h; Heating / reflux;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED
Patent: WO2008/57940 A1, 2008 ;
Location in patent: Page/Page column 61-62 ;
反应条件
1: With 1,1'-carbonyldiimidazole in dichloromethane T=20°C; 2: With hydrazine hydrate in dichloromethane T=20°C;
参考文献
BAYER SCHERING PHARMA AKTIENGESELLSCHAFT; VENNEMANN, Matthias; BAeR, Thomas; MAIER, Thomas; HOeLDER, Swen; BENEKE, Gerrit; DEHMEL, Florian; ZUeLCH, Armin; STRUB, Andreas; BECKERS, Thomas; INCE, Stuart; REHWINKEL, Hartmut; LIU, Ningshu; BOeMER, Ulf
Patent: WO2010/91824 A1, 2010 ;
Location in patent: Page/Page column 75 ;
WO 2010/091824 A1
反应条件
boron dimethyl-trifluoro sulphide in tetrahydrofuran T=20°C; 14 h;
参考文献
EP1961750 A1, ;
Page/Page column 90 ;