反应条件
1.1: potassium hydroxide / methanol / 5 - 25 °C
1.2: 0.5 h
2.1: sodium hydrogencarbonate / ethyl acetate
2.2: 20 °C
2.3: 80 °C / Inert atmosphere
3.1: dichloro bis(acetonitrile) palladium(II) / acetonitrile / 20 - 80 °C / Inert atmosphere
4.1: triethylamine / dichloromethane / 0 - 20 °C
5.1: hydrogen / 5 palladium on charcoal / tetrahydrofuran / 96 h / 50 °C / 2250.23 - 3000.3 Torr / autoclave; Inert atmosphere
View Scheme
参考文献
VERTEX PHARMACEUTICALS INCORPORATED; LOOKER, ADAM; Littler, Benjamin Joseph; Choudhury, Anusuya; Harrison, Cristian; Veluri, Ravikanth; Ryan, Michael P.; Jiang, Licong; Luss-Lusis, Eduard
Patent: US2013/116238 A1, 2013 ;