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Synthesis of amino-diamondoid pharmacophores via photocatalytic C–H aminoalkylation
Journal article   Open access   Peer reviewed

Synthesis of amino-diamondoid pharmacophores via photocatalytic C–H aminoalkylation

William K Weigel, Hoang T Dang, Hai-Bin Yang and David B C Martin
Chemical communications (Cambridge, England), Vol.56(67), pp.9699-9702
01/01/2020
DOI: 10.1039/d0cc02804e
PMCID: PMC7442722
PMID: 32699866
url
https://www.ncbi.nlm.nih.gov/pmc/articles/7442722View
Open Access

Abstract

We report a direct C–H aminoalkylation reaction using two light-activated H-atom transfer catalyst systems that enable the introduction of protected amines to native adamantane scaffolds with C–C bond formation. The scope of adamantane and imine reaction partners is broad and deprotection provides versatile amine and amino acid building blocks. Using readily available chiral imines, the enantioselective synthesis of the saxagliptin core and rimantadine derivatives is also described.
Optimization Synthesis Amines Imines Diamonds Enantiomers Covalent bonds

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