2-甲基-3-吗啉代丙酰肼 、 7-[1-(tert-butoxycarbonyl)piperidin-4-yl]-5-oxo-4,5-dihydropyrazolo[1,5-a]pyrimidine-3-carboxylic acid 在
N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下,
以
N,N-二甲基甲酰胺 为溶剂,
反应 16.0h,
以52%的产率得到tert-butyl 4-[3-({2-[2-methyl-3-(morpholin-4-yl)propanoyl]hydrazinyl}carbonyl)-5-oxo-4,5-dihydropyrazolo[1,5-a]pyrimidin-7-yl]piperidine-1-carboxylate