5-(氯甲基)-4-甲基-2-[4-(三氟甲基)苯基]-1,3-噻唑合成路线 (共 12 条)
反应条件
1: With methanesulfonyl chloride in dichloromethane T=0°C; 2 h; 2: With methanesulfonyl chloride; triethylamine T=0°C; 2 h;
参考文献
SMITHKLINE BEECHAM CORPORATION
Patent: WO2004/785 A2, 2003 ;
Location in patent: Page 43 ;
WO 2004/000785 A2
反应条件
methanesulfonyl chloride; triethylamine in dichloromethane T=0°C;
参考文献
KALYPSYS, INC.
Patent: WO2005/60958 A1, 2005 ;
Location in patent: Page/Page column 116 ;
WO 2005/060958 A1
反应条件
triethylamine in tetrahydrofuran
参考文献
Cheng, Xue-Min; Erasga, Noe; Filzen, Gary Frederick; Geyer, Andrew; Lee, Chitase; Trivedi, Bharat Kalidas
Patent: US2003/207924 A1, 2003 ;
反应条件
1: 87 percent / Pd(PPh3)4; K2CO3 / toluene / 100 °C 2: 70 percent / PdCl2(PPh3)2 / N,N-dimethyl-acetamide / 18 h / 140 °C 3: ClSO2Me; Et3N / CH2Cl2 View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 16, # 1 p. 49 - 54
反应条件
1: 70 percent / PdCl2(PPh3)2 / N,N-dimethyl-acetamide / 18 h / 140 °C 2: ClSO2Me; Et3N / CH2Cl2 View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 16, # 1 p. 49 - 54
反应条件
1.1: n-BuLi / tetrahydrofuran / -78 °C 1.2: tetrahydrofuran 2.1: 87 percent / Pd(PPh3)4; K2CO3 / toluene / 100 °C 3.1: 70 percent / PdCl2(PPh3)2 / N,N-dimethyl-acetamide / 18 h / 140 °C 4.1: ClSO2Me; Et3N / CH2Cl2 View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 16, # 1 p. 49 - 54
反应条件
1: 68 percent / Pd2(dba)3; AsPh3 / 1-methyl-pyrrolidin-2-one / 24 h / 70 °C 2: 70 percent / PdCl2(PPh3)2 / N,N-dimethyl-acetamide / 18 h / 140 °C 3: ClSO2Me; Et3N / CH2Cl2 View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 16, # 1 p. 49 - 54
反应条件
1: 70 percent / ethanol / Heating 2: 90 percent / LiAlH4 / tetrahydrofuran / 20 °C 3: 90 percent / MeSO2Cl; Et3N / CH2Cl2 / 0 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 13, # 9 p. 1517 - 1521
反应条件
1: 90 percent / LiAlH4 / tetrahydrofuran / 20 °C 2: 90 percent / MeSO2Cl; Et3N / CH2Cl2 / 0 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 13, # 9 p. 1517 - 1521
反应条件
caesium carbonate in acetonitrile T=20°C; Williamson reaction; 16 h;
参考文献
Pereira, Raquel; Gaudon, Claudine; Iglesias, Beatriz; Germain, Pierre; Gronemeyer, Hinrich; De Lera, Angel R.
Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 1 p. 49 - 54