Key points are not available for this paper at this time.
A second-generation route to the cereblon fragment of ARV-471, vepdegestrant, an orally available proteolysis targeting chimera (PROTAC) submitted to the FDA for NDA review to treat metastatic breast cancer, is reported. With the new, more convergent route, the chiral cyclic imide moiety is installed as a key fragment via reductive amination with a linker fragment.
Bernhardson et al. (Mon,) studied this question.
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