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Ligand-Enabled ?-C-H Arylation of ?-Amino Acids Without Installing Exogenous Directing Groups.


ABSTRACT: Herein we report acid-directed ?-C(sp3 )-H arylation of ?-amino acids enabled by pyridine-type ligands. This reaction does not require the installation of an exogenous directing group, is scalable, and enables the preparation of Fmoc-protected unnatural amino acids in three steps. The pyridine-type ligands are crucial for the development of this new C(sp3 )-H arylation.

SUBMITTER: Chen G 

PROVIDER: S-EPMC5302090 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature

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Ligand-Enabled β-C-H Arylation of α-Amino Acids Without Installing Exogenous Directing Groups.

Chen Gang G   Zhuang Zhe Z   Li Gen-Cheng GC   Saint-Denis Tyler G TG   Hsiao Yi Y   Joe Candice L CL   Yu Jin-Quan JQ  

Angewandte Chemie (International ed. in English) 20170103 6


Herein we report acid-directed β-C(sp<sup>3</sup> )-H arylation of α-amino acids enabled by pyridine-type ligands. This reaction does not require the installation of an exogenous directing group, is scalable, and enables the preparation of Fmoc-protected unnatural amino acids in three steps. The pyridine-type ligands are crucial for the development of this new C(sp<sup>3</sup> )-H arylation. ...[more]

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