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Scale up synthesis of IID572: A new β-lactamase inhibitor

Furegati, Markus and Nocito, Sandro and Reck, Folkert and Casarez, Anthony and Simmons, Robert and Koch, Guido and Schuetz, Heiner (2020) Scale up synthesis of IID572: A new β-lactamase inhibitor. Organic process research & development, 24. pp. 1244-1253.

Abstract

The new potentially best-in-class β-lactamase inhibitor IID572 was discovered by a late stage functionalization approach. An alternative scalable synthesis was developed to satisfy the short-term need for tox studies. The two key features were an intramolecular azomethine ylide [2+3] cycloaddition that allowed the quick formation of molecular complexity from cheap starting material and an efficient enzymatic resolution that resulted in high optical purity of a key intermediate.

Item Type: Article
Keywords: β-lactamase inhibitors, diazabicyclooctane, DBOs, scale-up, enzymatic resolution, [2+3] cycloaddition
Date Deposited: 19 Aug 2020 00:45
Last Modified: 19 Aug 2020 00:45
URI: https://oak.novartis.com/id/eprint/41817

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