Scale-Up Synthesis of IID572: A New β‑Lactamase
Inhibitor
Posted on 2020-06-18 - 16:05
The new potentially best-in-class
β-lactamase inhibitor IID572
was discovered by a late-stage functionalization approach. An alternative
synthesis was developed to satisfy the short-term material need for
toxicological studies in animals. The new synthetic strategy was built
on two key features, an intramolecular azomethine ylide [3 + 2] cycloaddition
that allowed the efficient formation of molecular complexity from
readily available starting materials and an enzymatic resolution that
resulted in high optical purity of a key intermediate.
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Furegati, Markus; Nocito, Sandro; Reck, Folkert; Casarez, Anthony; Simmons, Robert; Schuetz, Heiner; et al. (2020). Scale-Up Synthesis of IID572: A New β‑Lactamase
Inhibitor. ACS Publications. Collection. https://doi.org/10.1021/acs.oprd.0c00069
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AUTHORS (7)
MF
Markus Furegati
SN
Sandro Nocito
FR
Folkert Reck
AC
Anthony Casarez
RS
Robert Simmons
HS
Heiner Schuetz
GK
Guido Koch