1-Boc-氮杂环丁烷-3-羧酸合成路线 （共 19 条）
反应条件
1: With 4-methyl-morpholine in tetrahydrofuran T=-10°C; 0.25 h; 2: With sodium tetrahydroborate in tetrahydrofuran; water
参考文献
WO2005/28474 A2, ;
Page/Page column 219 ;
WO 2005/028474 A2
反应条件
lithium borohydride; triethylamine in tetrahydrofuran
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 18, # 20 p. 5581 - 5585
反应条件
1,3-Diiodo-5,5-dimethyl-2,4-imidazolidinedione in 1,2-dichloro-ethane 3 h; RefluxIrradiation; Product distribution / selectivity;
参考文献
TECHNION RandD FOUNDATION LTD.; NISNEVICH, Gennady; GANDELMAN, Mark; KULBITSKI, Kseniya
Patent: WO2011/154953 A1, 2011 ;
Location in patent: Page/Page column 28-30 ;
反应条件
1: NEt3 / tetrahydrofuran / 0.67 h / 0 °C 2: LiBH4 / tetrahydrofuran / 12 h / 20 °C 3: 1.11 g / oxalyl chloride; DMSO; NEt3 / CH2Cl2 / -78 - 20 °C View Scheme
参考文献
European Journal of Medicinal Chemistry, , vol. 34, # 5 p. 363 - 380
反应条件
1: 3-carboxyazetidine-1-carboxylic acid tert-butyl ester With dicyclohexyl-carbodiimide in tetrahydrofuran
T=20°C;
2: O,N-dimethyl-hydroxylamine hydrochloride With triethylamine in tetrahydrofuran; acetonitrile
T=20°C; 24 h;
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
1: 3-carboxyazetidine-1-carboxylic acid tert-butyl ester With N-ethyl-N,N-diisopropylamine; 1,1'-carbonyldiimidazole in tetrahydrofuran
T=20°C; 0.5 h;
2: N,O-dimethyl-hydroxylamine in tetrahydrofuran
T=20°C; 15 h;
参考文献
GAWECO, Anderson; WALKER, John; MONAHAN, Joseph, B.; CUBBAGE, Jerry, W.; CARROLL, Jeffery
Patent: WO2012/9649 A1, 2012 ;
Location in patent: Page/Page column 92-93 ;
反应条件
1: 4-(N,N-dimethlyamino)pyridine; dicyclohexyl-carbodiimide / dichloromethane / 17 h / 20 °C
2: acetic acid / 1,4-dioxane; water / 0.5 h / 100 - 110 °C / Microwave irradiation
View Scheme
参考文献
FAB PHARMA SAS; GERUSZ, Vincent; ESCAICH, Sonia; OXOBY, Mayalen; DENIS, Alexis
Patent: WO2011/61214 A1, 2011 ;
WO 2011/061214 A1
参考文献
ASTRAZENECA AB
Patent: WO2006/73361 A1, 2006 ;
Location in patent: Page/Page column 171 ;
WO 2006/073361 A1
反应条件
ammonium acetate; N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate in N,N-dimethyl-formamide
T=20°C;
参考文献
Incyte Corporation; Li, Yun-Long; Zhu, Wenyu; Mei, Song; Glenn, Joseph
Patent: US2014/121198 A1, 2014 ;
Location in patent: Paragraph 0688; 0689 ;
