tert-butyl N-methyl-N-sulfamoylcarbamate 、 (S)-2-(((3aR,4R,6R,6aR)-6-(4-((tert-butoxycarbonyl)(cyclopentyl)amino)-6-chloro-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-2,2-dimethyltetrahydrofuro[3,4-d][1,3]dioxol-4-yl)methoxy)-2-(diethoxyphosphoryl)-3-methoxypropanoic acid 在
sodium hydride 、
N-甲基吗啉 、 N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate 作用下,
以
N,N-二甲基甲酰胺 为溶剂,
以60 mg的产率得到tert-butyl (1-((3aR,4R,6R,6aR)-6-((((S)-1-((N-(tert-butoxycarbonyl)-N-methylsulfamoyl)amino)-2-(diethoxyphosphoryl)-3-methoxy-1-oxopropan-2-yl)oxy)methyl)-2,2-dimethyltetrahydrofuro[3,4-d][1,3]dioxol-4-yl)-6-chloro-1H-pyrazolo[3,4-d]pyrimidin-4-yl)(cyclopentyl)carbamate