[(6-甲基-3-吡啶基)氧基]乙酸 、 methyl (1S)-1-[({(1S,3S,4S)-4-{[(2S)-2-amino-3,3-dimethylbutanoyl]amino}-3-hydroxy-5-phenyl-1-[4-(2-pyridinyl)benzyl]pentyl}amino)carbonyl]-2,2-dimethylpropylcarbamate trifluoroacetate 在
N,N-二异丙基乙胺 、
3-(二乙氧基邻酰氧基)-1,2,3-苯并三嗪-4-酮 作用下,
以
四氢呋喃 为溶剂,
反应 18.0h,
以52%的产率得到methyl (1S)-1-[({(1S,3S,4S)-4-{[(2S)-3,3-dimethyl-2-({[(6-methyl-3-pyridinyl)oxy]acetyl}amino)butanoyl]amino}-3-hydroxy-5-phenyl-1-[4-(2-pyridinyl)benzyl]pentyl}amino)carbonyl]-2,2-dimethylpropylcarbamate