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Process Development for the Synthesis of a Monobactam Antibiotic—LYS228
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-02-20 , DOI: 10.1021/acs.oprd.9b00330 Zhongbo Fei 1 , Quanbing Wu 1 , Wanben Gong 1 , Peng Fu 1 , Cheng Li 1 , Xianwen Wang 1 , Yufeng Han 1 , Bin Li 1 , Lei Li 1 , Bin Wu 1 , Yi Zhao 1 , Jinjing Li 1 , Wenya Zhu 1 , Wenlong Qiu 1 , Jing Guo 1 , Jianguang Zhou 1 , Yuanqiang Li 2 , Marco Villa 3 , Chi Ming Cheung 1
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-02-20 , DOI: 10.1021/acs.oprd.9b00330 Zhongbo Fei 1 , Quanbing Wu 1 , Wanben Gong 1 , Peng Fu 1 , Cheng Li 1 , Xianwen Wang 1 , Yufeng Han 1 , Bin Li 1 , Lei Li 1 , Bin Wu 1 , Yi Zhao 1 , Jinjing Li 1 , Wenya Zhu 1 , Wenlong Qiu 1 , Jing Guo 1 , Jianguang Zhou 1 , Yuanqiang Li 2 , Marco Villa 3 , Chi Ming Cheung 1
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A scalable process for the novel monobactam antibiotic LYS228 has been developed. This paper covers a novel scalable process for producing β-lactam 10 in the multiple kilogram scale. An alternative approach to compound 7 without protecting-group exchange has been demonstrated to enable a shortened synthesis. A scalable process for the side chain 20, which used an alternative reagent to mitigate a safety risk from the initial med-chem approach, was performed. The final assembling to LYS228, a stable isolated product, was identified and executed in the multiple kilogram scale.
中文翻译：
合成单杆菌素LYS228的工艺开发
已经开发出可扩展的新型单杆菌素抗生素LYS228的方法。本文介绍了一种新颖的可扩展工艺，用于生产多千克规模的β-内酰胺10。已证明无需保护基交换的化合物7的替代方法可缩短合成时间。进行了侧链20的可扩展过程，该过程使用替代试剂来减轻初始医学化学方法带来的安全风险。最终组装成稳定的隔离产品LYS228，并以千克为单位进行了组装。
更新日期：2020-02-21
中文翻译：
合成单杆菌素LYS228的工艺开发
已经开发出可扩展的新型单杆菌素抗生素LYS228的方法。本文介绍了一种新颖的可扩展工艺，用于生产多千克规模的β-内酰胺10。已证明无需保护基交换的化合物7的替代方法可缩短合成时间。进行了侧链20的可扩展过程，该过程使用替代试剂来减轻初始医学化学方法带来的安全风险。最终组装成稳定的隔离产品LYS228，并以千克为单位进行了组装。
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