5-(4-溴苯基)-1-甲基-1H-吡唑合成路线 （共 5 条）
反应条件
sodium hydride in tetrahydrofuran
T=23°C; 3 h; Inert atmosphere; Overall yield = 90 percent; Overall yield = 1 g;
参考文献
GENESTE, Hervé; TURNER, Sean Colm; OCHSE, Michael; DRESCHER, Karla; BLACK, Lawrence A.; JANTOS, Katja
Patent: US2014/148461 A1, 2014 ;
Location in patent: Paragraph 0343-0344 ;
反应条件
1: para-bromoacetophenone; N,N-dimethyl-formamide dimethyl acetal in N,N-dimethyl-formamide
T=110°C; 4 h;
2: methylhydrazine in tert-butyl methyl ether
T=25°C; Product distribution / selectivity;
参考文献
PFIZER INC.
Patent: WO2009/69044 A1, 2009 ;
Location in patent: Page/Page column 67-68 ;
WO 2009/069044 A1
反应条件
in N,N-dimethyl-formamide
T=20 - 75°C; 5 h; Product distribution / selectivity;
参考文献
Graneto, Mathew J.; Maddux, Todd M.; Masferrer, Jaime L.
Patent: US2008/125474 A1, 2008 ;
Location in patent: Page/Page column 14; 16 ;
反应条件
1.1: N,N-dimethyl-formamide / 80 °C
1.2: 2 h / 80 °C
2.1: sodium hydride / tetrahydrofuran / 3 h / 23 °C / |Inert atmosphere
View Scheme
参考文献
GENESTE, Hervé; TURNER, Sean Colm; OCHSE, Michael; DRESCHER, Karla; BLACK, Lawrence A.; JANTOS, Katja
Patent: US2014/148461 A1, 2014 ;
反应条件
1: N,N-dimethyl-formamide / 4 h / 110 °C
2: tert-butyl methyl ether / 16 h / 25 °C
View Scheme
参考文献
De Koning, Pieter D.; Murtagh, Lorraine; Lawson, Jon P.; Vonder Embse, Richard A.; Kunda, Sastry A.; Kong, Wei
Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1046 - 1051
