(2R,6R)-4-(8-cyanoquinolin-5-yl)-6-methylmorpholine-2-carboxylic acid 、
(3R,4S)-tert-butyl 3-amino-4-fluoropiperidine-1-carboxylate 在
O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、
N,N-二异丙基乙胺 作用下,
以
二氯甲烷 为溶剂,
以56.2%的产率得到tert-butyl (3R,4S)-3-[[(2R,6R)-4-(8-cyanoquinolin-5-yl)-6-methylmorpholine-2-carbonyl]amino]-4-fluoropiperidine-1-carboxylate