Stereoselective Synthesis of Ezetimibe via Cross-Metathesis of Homoallylalcohols and α‑Methylidene-β-Lactams
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https://figshare.com/articles/dataset/Stereoselective_Synthesis_of_Ezetimibe_via_Cross-Metathesis_of_Homoallylalcohols_and_Methylidene-_-Lactams/3640155
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资源简介:
Ru-catalyzed cross-metathesis
(CM) reaction between β-arylated
α-methylidene-β-lactams and terminal olefins was developed.
The CM reaction is effectively catalyzed with Hoveyda–Grubbs
second-generation catalyst affording corresponding α-alkylidene-β-aryl-β-lactams
in good isolated yields (41–83%) with exclusive Z-selectivity. The developed protocol was successfully applied for
stereoselective preparation of Ezetimibe, the commercial cholesterol
absorption inhibitor.
创建时间:
2016-08-29



