2-(甲氧基甲基)吡咯烷 、 3-[3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1H-1,2,4-triazol-1-yl]pyridine-4-carbonyl chloride 在
Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 、
N,N-二异丙基乙胺 作用下,
以
N,N-二甲基甲酰胺 为溶剂,
反应 2.0h,
以80%的产率得到5-(4-chlorophenyl)-2-{[1-(4-{[2-(methoxymethyl)pyrrolidin-1-yl]carbonyl}pyridin-3-yl)-1H-1,2,4-triazol-3-yl]methyl}-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one