2-BOC-氨基-6-氯吡啶合成路线 (共 13 条)
反应条件
1: 1,1-dimethylethyl[6-chloro-2-pyridinyl]carbamate With n-butyllithium; N,N,N',N,-tetramethylethylenediamine in tetrahydrofuran; hexane
T=-78°C;
2: 1-bromo-4-chloro-butane in tetrahydrofuran
Heating; Further stages.;
参考文献
Davies, Antony J.; Brands, Karel M. J.; Cowden, Cameron J.; Dolling, Ulf-H.; Lieberman, David R.
Tetrahedron Letters, 2004 , vol. 45, # 8 p. 1721 - 1724
反应条件
1: 1,1-dimethylethyl[6-chloro-2-pyridinyl]carbamate With n-butyllithium; N,N,N',N,-tetramethylethylenediamine in tetrahydrofuran
T=-78°C; 2.83333 h; Inert atmosphere;
2: 1-benzyloxycarbonyl-piperidin-4-one in tetrahydrofuran
T=-78 - 40°C; Inert atmosphere;
3: With water; sodium hydrogencarbonate in tetrahydrofuran
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Patent: US2012/149698 A1, 2012 ;
Location in patent: Page/Page column 26 ;
反应条件
1.1: N,N,N',N,-tetramethylethylenediamine; n-butyllithium / tetrahydrofuran / -78 - -10 °C / Inert atmosphere
1.2: -78 - 20 °C
2.1: hydroxylamine hydrochloride; sodium acetate / ethanol; water / 4 h / 20 °C
3.1: hydrogenchloride / 1,4-dioxane / 0.5 h
4.1: trifluoroacetic anhydride; pyridine / 1,4-dioxane / 0 - 60 °C
View Scheme
参考文献
BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
Patent: US2011/190316 A1, 2011 ;
US 20110190316 A1