1-(四氢-2H-吡喃-2-基)-4-(4,4,5,5-四甲基-1,3,2-二噁硼烷-2-基)-1H-吲唑合成路线 (共 12 条)
反应条件
1: pyridinium p-toluenesulfonate / dichloromethane / 2 h / 50 °C
2: potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / dimethyl sulfoxide / 80 °C
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参考文献
Genentech, Inc.; Heald, Robert Andrew; McLean, Neville James
Patent: US2014/65136 A1, 2014 ;
反应条件
1.1: potassium acetate; acetic anhydride / ethylene glycol dimethyl ether / 6 h / 20 °C / |Inert atmosphere; |Large scale
1.2: 15 h / 60 °C / |Inert atmosphere; |Large scale
1.3: 0 °C / |Inert atmosphere; |Large scale
2.1: pyridinium p-toluenesulfonate / toluene; n-heptane / 11 h / 40 °C / |Inert atmosphere; |Large scale
2.2: 3.5 h / 0 - 25 °C / |Inert atmosphere; |Large scale
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参考文献
Tian, Qingping; Cheng, Zhigang; Yajima, Herbert M.; Savage, Scott J.; Green, Keena L.; Humphries, Theresa; Reynolds, Mark E.; Babu, Srinivasan; Gosselin, Francis; Askin, David; Kurimoto, Isao; Hirata, Norihiko; Iwasaki, Mitsuhiro; Shimasaki, Yasuharu; Miki, Takashi
Organic Process Research and Development, 2013 , vol. 17, # 1 p. 97 - 107