3-[(2-氟-4-碘苯基)氨基]-4-吡啶羧酸合成路线 （共 3 条）
反应条件
1: 1-amino-2-fluoro-4-iodobenzene With lithium hexamethyldisilazane in tetrahydrofuran
T=-65 - -55°C; 0.5 h;
2: 3-fluoro-4-pyridinecarboxylic acid in tetrahydrofuran
T=20°C; 96 h;
3: With hydrogenchloride in water
pH=2;
参考文献
APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.
Patent: WO2007/123936 A1, 2007 ;
Location in patent: Page/Page column 36 ;
WO 2007/123936 A1
反应条件
1: 1-amino-2-fluoro-4-iodobenzene With lithium hexamethyldisilazane in tetrahydrofuran
T=-55°C; Inert atmosphere;
2: 3-fluoro-4-pyridinecarboxylic acid in tetrahydrofuran
T=20°C; 96 h;
3: With hydrogenchloride in water
pH=2;
参考文献
MERCK SERONO S.A.; GOUTOPOULOS, Andreas; YU, Henry; ASKEW, Benny, C.; LIU-BUJALSKI, Lesley
Patent: WO2010/17051 A1, 2010 ;
Location in patent: Page/Page column 26-27 ;
反应条件
1: 1-amino-2-fluoro-4-iodobenzene With lithium hexamethyldisilazane in tetrahydrofuran
T=-67 - -59°C; 2.5 h;
2: 2-fluoropyridine-4-carboxylic acid in tetrahydrofuran
T=-59 - 20°C; 96 h;
3: With hydrogenchloride; sodium hydroxide; water
Product distribution / selectivity; more than 3 stages;
参考文献
APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.
Patent: WO2006/45514 A1, 2006 ;
Location in patent: Page/Page column 34 ;
WO 2006/045514 A1
