3,3-difluoropyrrolidine-1-carbonyl chloride 、 (1R,2S,5S)-3-[(2S)-2-amino-3,3-dimethyl-butanoyl]-N-[(1S)-2-amino-2-oxo-1-[[(6R)-5-oxo-4-azaspiro[2.4]heptan-6-yl]methyl]ethyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide hydrochloride 在
N,N-二异丙基乙胺 作用下,
以
四氢呋喃 为溶剂,
以70 mg的产率得到(1R,2S,5S)-N-[(1S)-2-amino-2-oxo-1-[[(6R)-5-oxo-4-azaspiro[2.4]heptan-6-yl]methyl]ethyl]-3-[(2S)-2-[(3,3-difluoropyrrolidine-1-carbonyl)amino]-3,3-dimethylbutanoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide