4-(6-(溴甲基)-2-氯噻吩并[3,2-d]嘧啶-4-基)吗啉合成路线 （共 6 条）
反应条件
phosphorus tribromide in benzene
1 h; Heating / reflux;
参考文献
GENENTECH, INC.; PIRAMED LIMITED; CASTANEDO, Georgette; DOTSON, Jennafer; GOLDSMITH, Richard; GUNZNER, Janet; HEFFRON, Tim; MATHIEU, Simon; OLIVERO, Alan; STABEN, Steven; SUTHERLIN, Daniel P.; TSUI, Vickie; WANG, Shumei; ZHU, Bing-Yan; BAYLISS, Tracy; CHUCKOWREE, Irina; FOLKES, Adrian; WAN, Nan Chi
Patent: WO2008/73785 A2, 2008 ;
Location in patent: Page/Page column 161 ;
WO 2008/073785 A2
反应条件
1.1: methanol / 1 h / 20 °C
2.1: lithium diisopropyl amide / hexane; tetrahydrofuran / 1 h / -78 °C
2.2: 11 h / -78 - 20 °C
3.1: sodium tetrahydroborate; methanol / 1 h / 20 °C
4.1: triphenylphosphine; N-bromosuccinmide / dichloromethane / 3 h / 25 °C
View Scheme
参考文献
CURIS, INC.; BAO, Rudi; LAI, Chengjung; QIAN, Changgeng
Patent: WO2011/130628 A1, 2011 ;
WO 2011/130628 A1
反应条件
1.1: lithium diisopropyl amide / hexane; tetrahydrofuran / 1 h / -78 °C
1.2: 11 h / -78 - 20 °C
2.1: sodium tetrahydroborate; methanol / 1 h / 20 °C
3.1: triphenylphosphine; N-bromosuccinmide / dichloromethane / 3 h / 25 °C
View Scheme
参考文献
CURIS, INC.; BAO, Rudi; LAI, Chengjung; QIAN, Changgeng
Patent: WO2011/130628 A1, 2011 ;
WO 2011/130628 A1
反应条件
1: sodium tetrahydroborate; methanol / 1 h / 20 °C
2: triphenylphosphine; N-bromosuccinmide / dichloromethane / 3 h / 25 °C
View Scheme
参考文献
CURIS, INC.; BAO, Rudi; LAI, Chengjung; QIAN, Changgeng
Patent: WO2011/130628 A1, 2011 ;
WO 2011/130628 A1
反应条件
1.1: trichlorophosphate / 10 h / Reflux
2.1: methanol / 1 h / 20 °C
3.1: lithium diisopropyl amide / hexane; tetrahydrofuran / 1 h / -78 °C
3.2: 11 h / -78 - 20 °C
4.1: sodium tetrahydroborate; methanol / 1 h / 20 °C
5.1: triphenylphosphine; N-bromosuccinmide / dichloromethane / 3 h / 25 °C
View Scheme
参考文献
CURIS, INC.; BAO, Rudi; LAI, Chengjung; QIAN, Changgeng
Patent: WO2011/130628 A1, 2011 ;
WO 2011/130628 A1
反应条件
1.1: 2 h / 190 °C
1.2: Heating
2.1: trichlorophosphate / 10 h / Reflux
3.1: methanol / 1 h / 20 °C
4.1: lithium diisopropyl amide / hexane; tetrahydrofuran / 1 h / -78 °C
4.2: 11 h / -78 - 20 °C
5.1: sodium tetrahydroborate; methanol / 1 h / 20 °C
6.1: triphenylphosphine; N-bromosuccinmide / dichloromethane / 3 h / 25 °C
View Scheme
参考文献
CURIS, INC.; BAO, Rudi; LAI, Chengjung; QIAN, Changgeng
Patent: WO2011/130628 A1, 2011 ;
WO 2011/130628 A1
