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Stereoselective synthesis of chiral thiol-containing 1,2-aminoalcohols via SmI 2 -mediated coupling

Tetrahedron, ISSN: 0040-4020, Vol: 76, Issue: 51, Page: 131249
2020
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Article Description

The stereoselective synthesis of highly functionalized aminohydroxythiols represents a synthetic challenge as the oxidation sensitivity and coordinating property of the thiol group interferes with many established synthetic methods. The SmI 2 /LiBr-mediated reductive coupling between Ellman N -sulfinylimines, containing thiol groups protected either as trityl thioether or dihydrothiazolidine, and aldehydes enables the synthesis of chiral aminohydroxythiols in high enantio- and diastereoselectivity. The scope of this reaction has been established for 18 examples and applied for the synthesis of a complex intermediate needed for a biosynthesis study.

Bibliographic Details

Carina Doler; Michael Friess; Florian Lackner; Hansjörg Weber; Roland C. Fischer; Rolf Breinbauer

Elsevier BV

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics; Chemistry

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