1-甲苯磺酰基-1H-吡咯并[2,3-B]吡啶-3-基硼酸合成路线 （共 5 条）
反应条件
n-butyllithium in tetrahydrofuran T=-90 - -80°C; 0.5 h; Large scale;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; TAYLOR, Lori, Kell; SEWELL, Kathryn, Lea; HOOCK, Thomas, Carl
Patent: WO2014/74471 A1, 2014 ;
Location in patent: Paragraph 0275-0277 ;
反应条件
1: With n-butyllithium in tetrahydrofuran T=-78°C; 0.5 h; 2: With tri-isopropoxy-borane in tetrahydrofuran T=-78°C; 1 h;
参考文献
CELLTECH R and D LIMITED
Patent: WO2006/38001 A1, 2006 ;
Location in patent: Page/Page column 39 ;
WO 2006/038001 A1
反应条件
1.1: bromine / N,N-dimethyl-formamide / 2.67 h / 0 - 10 °C / |Large scale 2.1: sodium hydride / tetrahydrofuran / 10 - 20 °C / |Large scale 2.2: 1.5 h / 10 - 20 °C / |Large scale 3.1: n-butyllithium / tetrahydrofuran / 0.5 h / -90 - -80 °C / |Large scale View Scheme
反应条件
1.1: sodium hydride / tetrahydrofuran / 10 - 20 °C / |Large scale 1.2: 1.5 h / 10 - 20 °C / |Large scale 2.1: n-butyllithium / tetrahydrofuran / 0.5 h / -90 - -80 °C / |Large scale View Scheme
反应条件
in dichloromethane T=20 - 30°C; Large scale;
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; TAYLOR, Lori, Kell; SEWELL, Kathryn, Lea; HOOCK, Thomas, Carl
Patent: WO2014/74471 A1, 2014 ;
Location in patent: Paragraph 0278-0280 ;
