The New Route Design Of (S,S)-2,8-diazabicyclo [4.3.0] Nonane And Synthesis Of The Key Intermediate

Objective: To design and synthesize the key intermediate ofmoxifloxacin.Methods: A novel intermediate of moxifloxacin,(S)-N-benzyl-N-(1-benzyl-2,5-dioxopyrrolidin-3-yl)acrylamide, wasconstructed starting from L-aspartate and benzylamine by preparinganhydride,cyclization, deprotection,reprotection, acylation.Results: The target product was obtained with the first six-stepsof19%and it was characterized LC-MS and1HNMR;Conclusion: the new design route will benefit from cheapmaterials,convenient operations and mild conditions.