Wu, Quanbing, Li, Lei, Li, Bin, Chen, Like, Wu, Bin, Wang, Xianwen and Guo, Tina (2020) Process Development for the Synthesis of a -monobactam antibiotic - LYS228. Organic Process Research & Development, 24 (3). pp. 363-370. ISSN 1083-61601520-586X

Abstract

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.

Item Type:	Article
Date Deposited:	01 May 2020 00:45
Last Modified:	01 May 2020 00:45
URI:	https://oak.novartis.com/id/eprint/39705