反应条件
1.1: lithium diisopropyl amide / tetrahydrofuran / 1.5 h / -78 °C / |Inert atmosphere
1.2: 0.5 h / -78 °C / |Inert atmosphere
2.1: caesium carbonate / tetrahydrofuran / 60 °C / |Inert atmosphere
3.1: palladium 10 on activated carbon; triethylamine; hydrogen / tetrahydrofuran; methanol / 72 h / 2327.23 Torr / |Inert atmosphere
4.1: water; sodium hydroxide / 1 h / 20 - 25 °C
View Scheme
参考文献
GENENTECH, INC.; FORMA TM, LLC; BAIR, Kenneth W.; BAUMEISTER, Timm R.; BUCKMELTER, Alexandre J.; CLODFELTER, Karl H.; DRAGOVICH, Peter; GOSSELIN, Francis; GUNZNER-TOSTE, Janet; HAN, Bingsong; LIN, Jian; LIU, Xiongcai; REYNOLDS, Dominic J.; SMITH, Chase C.; WANG, Zhongguo; ZAK, Mark; ZHANG, Yamin; ZHAO, Guiling; ZHENG, Xiaozhang; YUEN, Po-Wai
Patent: WO2013/127266 A1, 2013 ;