(R)-3-bromo-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepine[5',6':4,5]furan[3,2-f]quinoline-8-one 、
2-chloro-6-(difluoromethyl)pyrimidin-4-amine 在
tris-(dibenzylideneacetone)dipalladium(0) 、
caesium carbonate 、
R-(+)-1,1'-联萘-2,2'-双二苯膦 作用下,
以
1,4-二氧六环 为溶剂,
生成 (R)-3-((2-chloro-6-(difluoromethyl)pyrimidin-4-yl)amino)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepine[5',6':4,5]furan[3,2-f]quinoline-8-one