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Org Lett. 2016 Nov 4;18(21):5512-5515. Epub 2016 Oct 19.

Metal-Free Direct Amidation of Naphthoquinones Using Hydroxamic Acids as an Amide Source: Application in the Synthesis of an HDAC6 Inhibitor.

Author information

1
Department of Applied Chemistry, China Agricultural University , 2 Yuanmingyuan West Road, Beijing 100193, China.
2
Department of Drug Discovery and Biomedical Sciences, Medical University of South Carolina , 280 Calhoun Street, MSC140 QF307, Charleston, South Carolina 29425, United States.

Abstract

A novel synthetic approach to amidoquinones by the reaction of naphthoquinones with hydroxamic acids under basic conditions was developed. The reaction is mild and operationally simple, and it affords high yields of amidoquinones. With this new method, a novel, very strong HDAC6 inhibitor, which showed high toxicity to AML cells, was successfully synthesized.

PMID:
27759399
PMCID:
PMC5242401
DOI:
10.1021/acs.orglett.6b02740
[Indexed for MEDLINE]
Free PMC Article

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