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Fluorinated Amine Stereotriads via Allene Amination
Journal article   Peer reviewed

Fluorinated Amine Stereotriads via Allene Amination

Lu Liu, Nels C Gerstner, Lucas J Oxtoby, Ilia A Guzei and Jennifer M Schomaker
Organic letters, Vol.19(12), pp.3239-3242
06/16/2017
DOI: 10.1021/acs.orglett.7b01342
PMCID: PMC5541934
PMID: 28573862
url
https://www.ncbi.nlm.nih.gov/pmc/articles/5541934View
Open Access

Abstract

The incorporation of fluorine into organic scaffolds often improves the bioactivity of pharmaceutically relevant compounds. C-F/C-N/C-O stereotriad motifs are prevalent in antivirals, neuraminidase inhibitors, and modulators of androgen receptors, but are challenging to install. An oxidative allene amination strategy using Selectfluor rapidly delivers triply functionalized triads of the form C-F/C-N/C-O, exhibiting good scope and diastereoselectivity for all syn products. The resulting stereotriads are readily transformed into fluorinated pyrrolidines and protected α-, β-, and γ-amino acids.
Alkadienes Amination Amines - chemistry Catalysis Molecular Structure Stereoisomerism

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