5-((Z)-(5-氟-2-氧代吲哚烷-3-亚基)甲基)-2,4-二甲基-1H-吡咯-3-羧酸合成路线 (共 13 条)
反应条件
(benzotriazo-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate; triethylamine in DMF (N,N-dimethyl-formamide) T=20°C; 2 h;
参考文献
PFIZER PRODUCTS INC.
Patent: WO2007/34272 A1, 2007 ;
Location in patent: Page/Page column 17-18 ;
WO 2007/034272 A1
反应条件
1: 5-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine in tetrahydrofuran T=20°C; 0.5 h; 2: 1-amino-2-diethylamino-ethane in tetrahydrofuran T=20°C;
参考文献
GENERICS [UK] LIMITED; MYLAN DEVELOPMENT CENTRE PRIVATE LIMITED; GAITONDE, Abhay; CHOUDHARI, Bharati; BANSODE, Prakash; PHADTARE, Sunanda
Patent: WO2010/1167 A2, 2010 ;
Location in patent: Page/Page column 50-51 ;
反应条件
1.1: thionyl chloride / N,N-dimethyl-formamide / toluene / 8 h / 70 °C 2.1: 2-methyl tetrahydrofuran / 1.08 h / 70 °C 2.2: pH 2 2.3: pH 8.5 View Scheme
参考文献
SCINOPHARM TAIWAN, LTD.; Henscheke, Julian P.; Chen, Yung-Fa
Patent: US2013/190512 A1, 2013 ;