2-溴-7-碘-5-甲苯磺酰基-5H-吡咯并[2,3-B]吡嗪合成路线 （共 5 条）
反应条件
1: 2-bromo-7-iodo-5H-pyrrolo[3,2-b]pyrazine With sodium hydride in tetrahydrofuran; mineral oil
T=0°C; 0.333333 h;
2: p-toluenesulfonyl chloride in tetrahydrofuran; mineral oil
T=20°C; 3 h;
参考文献
UNIVERSITY OF ROCHESTER; BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA; GELBARD, Harris A.; DEWHURST, Stephen; GENDELMAN, Howard E.
Patent: WO2014/85795 A1, 2014 ;
Location in patent: Paragraph 0284 ;
反应条件
sodium hydride in tetrahydrofuran
T=0 - 20°C; 3.33333 h;
参考文献
SGX PHARMACEUTICALS, INC.
Patent: WO2006/15124 A2, 2006 ;
Location in patent: Page/Page column 103 ;
WO 2006/015124 A2
反应条件
1.1: pyridine / tetrahydrofuran / 96 h
2.1: tetrabutyl ammonium fluoride / tetrahydrofuran / 20 h / 75 °C
3.1: N-iodo-succinimide / acetone / 4 h / 20 °C
4.1: sodium hydride / tetrahydrofuran; mineral oil / 0.33 h / 0 °C
4.2: 3 h / 20 °C
View Scheme
参考文献
UNIVERSITY OF ROCHESTER; GELBARD, Harris, A.; DEWHURST, Stephen; GOODFELLOW, Val, S.; WIEMANN, Torsten; RAVULA, Satheesh, Babu; LOWETH, Colin, J.
Patent: WO2011/149950 A2, 2011 ;
WO 2011/149950 A2
反应条件
1.1: tetrabutyl ammonium fluoride / tetrahydrofuran / 20 h / 75 °C
2.1: N-iodo-succinimide / acetone / 4 h / 20 °C
3.1: sodium hydride / tetrahydrofuran; mineral oil / 0.33 h / 0 °C
3.2: 3 h / 20 °C
View Scheme
参考文献
UNIVERSITY OF ROCHESTER; GELBARD, Harris, A.; DEWHURST, Stephen; GOODFELLOW, Val, S.; WIEMANN, Torsten; RAVULA, Satheesh, Babu; LOWETH, Colin, J.
Patent: WO2011/149950 A2, 2011 ;
WO 2011/149950 A2
反应条件
1.1: N-iodo-succinimide / acetone / 4 h / 20 °C
2.1: sodium hydride / tetrahydrofuran; mineral oil / 0.33 h / 0 °C
2.2: 3 h / 20 °C
View Scheme
参考文献
UNIVERSITY OF ROCHESTER; GELBARD, Harris, A.; DEWHURST, Stephen; GOODFELLOW, Val, S.; WIEMANN, Torsten; RAVULA, Satheesh, Babu; LOWETH, Colin, J.
Patent: WO2011/149950 A2, 2011 ;
WO 2011/149950 A2
