3,4-dichloro-6-[2-(dimethylphosphoryl)pyrimidin-5-yl]-7-fluoro-2-methyl-1,5-naphthyridine 、
(R)-3-(1-氨基丙基)苯甲腈盐酸盐 在
tris-(dibenzylideneacetone)dipalladium(0) 、 [2'-(diphenylphosphanyl)-[1,1'-binaphthalen]-2-yl]diphenylphosphane 、
caesium carbonate 作用下,
以
甲苯 为溶剂,
以19 %的产率得到3-[(1R)-1-({3-chloro-6-[2-(dimethylphosphoryl)pyrimidin-5-yl]-7-fluoro-2-methyl-1,5-naphthyridin-4-yl}amino)propyl]benzonitrile