Five-Step Enantioselective Synthesis of Islatravir via Asymmetric Ketone Alkynylation and an Ozonolysis Cascade.

CHEMISTRY-A EUROPEAN JOURNAL(2020)

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摘要
A 5-step enantioselective synthesis of the potent anti-HIV nucleoside islatravir is reported. The highly efficient route was enabled by a novel enantioselective alkynylation of an a,b-unsaturated ketone, a unique ozonolysis-dealkylation cascade in water, and an enzymatic aldol-glycosylation cascade.
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关键词
asymmetric alkynylation,biocatalysis,ozonolysis,synthesis
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