4'-[(2S)-2-{[(trans-4-{[(tert-butoxycarbonyl)amino]methyl}cyclohexyl)carbonyl]amino}-3-oxo-3-{[4-(2H-tetrazol-5-yl)phenyl] amino}propyl]-2-methylbiphenyl-4-carboxylic acid 、
methyl 5-amino-6-oxopiperidine-2 carboxylate 在
N,N-二异丙基乙胺 、 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,
反应 16.0h,
以31%的产率得到methyl 5-[({4'-[(2S)-2-{[(trans-4-{[(tert-butoxycarbonyl)amino]methyl}cyclohexyl)carbonyl]amino}-3-oxo-3-{ [4-(1H-tetrazol-5-yl)phenyl]amino}propyl]-2-methylbiphenyl-4-yl}carbonyl)amino]-6-oxopiperidin-2-carboxylate