Journal
TETRAHEDRON
Volume 72, Issue 52, Pages 8584-8592Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2016.11.039
Keywords
Malonamic esters; Alkylation; Trifunctional compounds; Suberoylanilide hydroxamic acid; Histone deacetylase inhibitors
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Funding
- Mandeville Trust
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Alkylation of malonamic esters provides a direct approach to derivatives of suberoylanilide hydroxamic acid (SAHA) that are branched at the amide carbon atom, a location pivotal for enhancing biological and therapeutic activity. Alkylations use NaH in THE followed by addition of the ester of 6-bromohexanoic acid; no protection of the amidic NH group is necessary. By this means, carboxylic acid, ester, amide, hydroxymethyl and 2-benzimidazolyl branching units have been appended to the SAHA backbone. Routes to vary one of the branching units at a time have been developed. (C) 2016 Elsevier Ltd. All rights reserved.
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