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A new synthesis of LYS228, fitting for further process development for commercial manufacture, is described. The key features of this synthesis include development of new protocols for acylation reactions, application of an asymmetric hydrogenation via dynamic kinetic resolution, and a late-stage ring closure to form β-lactam 1.

Citation

Zhongbo Fei, Quanbing Wu, Lei Li, Qun Jiang, Bin Li, Like Chen, Hao Wang, Bin Wu, Xianwen Wang, Feng Gao, Wenlong Qiu, Jing Guo, Chi Ming Cheung. New Synthesis for the Monobactam Antibiotic-LYS228. The Journal of organic chemistry. 2020 Jun 05;85(11):6854-6861

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PMID: 32408741

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