2-氨基-N-(2-氯-6-甲基苯基)噻唑-5-甲酰胺合成路线 （共 10 条）
反应条件
1: (E)-N-(2-chloro-6-methylphenyl)-3-ethoxyacrylamide With N-bromosuccinmide in 1,4-dioxane; water T=-10 - 22°C; 3 h; 2: thiourea in 1,4-dioxane; water T=100°C; 2 h; 3: With ammonia in 1,4-dioxane; water T=20 - 22°C;
参考文献
WO2008/76883 A2, ;
Page/Page column 53-54 ;
WO 2008/076883 A2
反应条件
1: (E)-N-(2-chloro-6-methylphenyl)-3-ethoxyacrylamide With N-bromosuccinmide in 1,4-dioxane; water T=-10 - 22°C; 3 h; 2: thiourea in 1,4-dioxane; water T=80°C; 2 h;
参考文献
WO2005/77945 A2, ;
Page/Page column 51 ;
WO 2005/077945 A2
反应条件
1: With hydrogenchloride; acetic acid T=50 - 65°C; 11 h; Industry scale; 2: With sodium methylate in methanol pH=8 - 9; Industry scale;
参考文献
US2007/37978 A1, ;
Page/Page column 3 ;
反应条件
trifluoroacetic acid in dichloromethane
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 13, # 22 p. 4007 - 4010
Bioorganic and Medicinal Chemistry Letters, , vol. 14, # 24 p. 6061 - 6066
反应条件
1: i-Pr2NEt / tetrahydrofuran 2: TFA / CH2Cl2 View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 14, # 24 p. 6061 - 6066
反应条件
1: N-bromosuccinmide; water / 1,4-dioxane / 3 h / -10 - 22 °C 2: 1,4-dioxane; water / 2 h / 80 °C View Scheme
参考文献
Archiv der Pharmazie, , vol. 344, # 7 p. 451 - 458
反应条件
in 1,4-dioxane; water T=80°C; 2 h;
参考文献
Archiv der Pharmazie, , vol. 344, # 7 p. 451 - 458
反应条件
potassium carbonate; palladium diacetate; 2,2'-bis-(diphenylphosphino)-1,1'- binaphthyl T=100 - 110°C; 20 h;
参考文献
BRISTOL-MYERS SQUIBB COMPANY
Patent: WO2005/77945 A2, 2005 ;
Location in patent: Page/Page column 54-55 ;
WO 2005/077945 A2
反应条件
1: With sodium t-butanolate in tetrahydrofuran T=10 - 20°C; 1.5 h; 2: With hydrogenchloride in tetrahydrofuran; water T=0 - 5°C; 1.75 h;
参考文献
WO2005/77945 A2, ;
Page/Page column 51-52 ;
WO 2005/077945 A2
反应条件
1: NaNO2; CuBr 2: NaH View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 14, # 24 p. 6061 - 6066
