(R)-2-氯-A-甲基-苯甲胺 、 3,4-dichloro-6-[6-(dimethylphosphoryl)pyridin-3-yl]-7-fluoro-2-methyl-1,5-naphthyridine 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62 %的产率得到3-chloro-N-[(1R)-1-(2-chlorophenyl)ethyl]-6-[6-(dimethylphosphoryl)pyridin-3-yl]-7-fluoro-2-methyl-1,5-naphthyridin-4-amine