RESEARCH ARTICLE


Solid Phase Syntheses of Ferulic Acid Derivatives Acetyl Feruloyl Tyrosine and Acetyl Feruloyl Valyl Tyrosine



Dongxin Zhao1, *, Li Ma1, Kui Lu1, 2, *, Juan He1
1 School of Chemistry and Chemical Engineering, Henan University of Technology, Zhengzhou 450001, China
2 School of Material and Chemical Engineering, Henan Institute of Engineering, Zhengzhou 450007, China


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© 2015 Zhao et al.

open-access license: This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 International Public License (CC-BY 4.0), a copy of which is available at: (https://creativecommons.org/licenses/by/4.0/legalcode). This license permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

* Address correspondence to this author at the Locus Street, Hi-Tech Industrial Development Zone, School of Chemistry and Chemical Engineering, Henan University of Technology, Zhengzhou 450001, P. R. China; Tel: +86-371-67756945; Fax: +86-371-67756718; E-mail: zhaodx798@163.com; lukui126@126.com


Abstract

Ferulic acid was used as a common drug for cardia-cerebrovascular disease and leukopenia, but the application of ferulic acid was inhibited by the poor absorption and stability. The improvement of these defects can be realized by modifying ferulic acid by amino acids, because the amido bond can increase the bioavailability and therapeutic effect of some drugs based on the peptide transporter system of mammalian which can transport the peptidyl drugs. The peptidyl derivatives of ferulic acid, namely acetyl feruloyl tyrosine and acetyl feruloyl valyl tyrosine, were synthesized using Fmoc solid-phase synthesis method. The synthesized ferulic acid amide derivatives were purified by RP-HPLC, and characterized by IR, HNMR and ESI-MS. The results indicated that Fmoc solid phase synthesis was a convenient method for the amide bond modification of ferulic acid and the further property research on ferulic acid derivatives.

Keywords: Derivative, ferulic acid, purification, solid phase, synthesis, tyrosine, valine.