3-环戊基-3-[4-(4,4,5,5-四甲基-1,3,2-二氧杂硼烷-2-基)-1H-吡唑-1-基]丙腈合成路线 （共 5 条）
反应条件
1,8-diazabicyclo[5.4.0]undec-7-ene in acetonitrile T=20°C; Inert atmosphereReflux;
参考文献
Zhou, Jiacheng; Liu, Pingli; Lin, Qiyan; Metcalf, Brian W.; Meloni, David; Pan, Yongchun; Xia, Michael; Li, Mei; Yue, Tai-Yuen; Rodgers, James D.; Wang, Haisheng
Patent: US2010/190981 A1, 2010 ;
Location in patent: Page/Page column 91 ;
US 20100190981 A1
反应条件
potassium acetate; tetrakis(triphenylphosphine) palladium(0) in 1,4-dioxane T=120°C; 3 h; microwave;
参考文献
BIOCRYST PHARMACEUTICALS, INC.; BABU, Yarlagadda S.; KOTIAN, Pravin L.; KUMAR, V. Satish; WU, Minwan; LIN, Tsu-Hsing
Patent: WO2011/31554 A2, 2011 ;
Location in patent: Page/Page column 148-149 ;
WO 2011/031554 A1
反应条件
1: potassium tert-butylate / tetrahydrofuran / 49 h / 0 - 20 °C 2: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile / 20 °C 3: potassium acetate / tetrakis(triphenylphosphine) palladium(0) / 1,4-dioxane / 3 h / 120 °C / microwave View Scheme
参考文献
BIOCRYST PHARMACEUTICALS, INC.; BABU, Yarlagadda S.; KOTIAN, Pravin L.; KUMAR, V. Satish; WU, Minwan; LIN, Tsu-Hsing
Patent: WO2011/31554 A2, 2011 ;
WO 2011/031554 A1
反应条件
1: 1,8-diazabicyclo[5.4.0]undec-7-ene / acetonitrile / 20 °C 2: potassium acetate / tetrakis(triphenylphosphine) palladium(0) / 1,4-dioxane / 3 h / 120 °C / microwave View Scheme
参考文献
BIOCRYST PHARMACEUTICALS, INC.; BABU, Yarlagadda S.; KOTIAN, Pravin L.; KUMAR, V. Satish; WU, Minwan; LIN, Tsu-Hsing
Patent: WO2011/31554 A2, 2011 ;
WO 2011/031554 A1
反应条件
Chiralpak.(R). IA in hexanes; ethanol T=20°C; Purification / work up;
参考文献
US2010/190981 A1, ;
Page/Page column 91-92 ;
US 20100190981 A1
