ethyl 2-[(trans)-7-chloro-5-(2,3-dimethoxyphenyl)-2-thioxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl]acetate 、
(3-hydrazino-2,2-dimethyl-3-oxopropyl)carbamic acid tert-butyl ester 在
acetonitrile-water 作用下,
以
1,4-二氧六环 为溶剂,
反应 72.0h,
以139 mg (19.7% of theory) of the racemic diastereomer 30A-1 and 134 mg (19.0% of theory) of the racemic diastereomer 30A-2 are obtained的产率得到[1-{2-[(tert-Butoxycarbonyl)amino]-1,1-dimethylethyl}-8-chloro-6-(2,3-dimethoxyphenyl)-4H,6H-[1,2,4]triazolo[4,3-a][4,1]benzoxazepin-4-yl]acetate ethyl ester