1,2,4-三氟-5-(甲基磺酰基)苯合成路线 （共 6 条）
反应条件
N-ethyl-N,N-diisopropylamine in N,N-dimethyl-formamide
T=20°C;
参考文献
ARRAY BIOPHARMA INC.; AICHER, Thomas Daniel; BENCSIK, Josef Roland; BOYD, Steven Armen; CONDROSKI, Kevin Ronald; FELL, Jay Bradford; FISCHER, John P.; HINKLIN, Ronald Jay; PRATT, Scott Alan; SINGH, Ajay; TURNER, Timothy M.
Patent: WO2011/146335 A1, 2011 ;
Location in patent: Page/Page column 59 ;
WO 2011/146335 A1
反应条件
1: 2,4,5-trifluorobenzenesulfinic acid With potassium carbonate in DMF (N,N-dimethyl-formamide)
0.0833333 h;
2: methyl iodide in DMF (N,N-dimethyl-formamide)
T=20°C; 60 h;
参考文献
Jolidon, Synese J.; Narquizian, Robert; Nettekoven, Matthias Heinrich; Norcross, Roger David; Pinard, Emmanuel; Stalder, Henri
Patent: US2005/209241 A1, 2005 ;
Location in patent: Page/Page column 28 ;
US 20050209241 A1
反应条件
1: 2,4,5-trifluorobenzenesulfonyl chloride With sodium hydrogencarbonate; sodium sulfite in water
T=150°C; 0.111111 h; Microwave;
2: monobromoacetic acid in water
T=150°C; 0.0833333 h; Microwave;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2005/121110 A1, 2005 ;
Location in patent: Page/Page column 139-140 ;
WO 2005/121110 A1
反应条件
SbF5
T=60°C; Substitution; 3 h;
参考文献
Olah; Orlinkov; Oxyzoglou; Prakash, G.K. Suria
Russian Journal of Organic Chemistry, 1998 , vol. 34, # 11 p. 1573 - 1578
反应条件
1.1: sodium hydroxide; sodium sulfite / water / pH 14
1.2: pH ~ 1 / Cooling with ice
2.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 20 °C
View Scheme
参考文献
ARRAY BIOPHARMA INC.; AICHER, Thomas Daniel; BENCSIK, Josef Roland; BOYD, Steven Armen; CONDROSKI, Kevin Ronald; FELL, Jay Bradford; FISCHER, John P.; HINKLIN, Ronald Jay; PRATT, Scott Alan; SINGH, Ajay; TURNER, Timothy M.
Patent: WO2011/146335 A1, 2011 ;
WO 2011/146335 A1
反应条件
trifluorormethanesulfonic acid; Boron tris(trifluoromethanesulfonate)
T=50°C; Substitution; 3 h;
参考文献
Olah; Orlinkov; Oxyzoglou; Prakash, G.K. Suria
Russian Journal of Organic Chemistry, 1998 , vol. 34, # 11 p. 1573 - 1578
