[Improved method of epalrestat synthesis]

Rong Sheng; Tao Liu; Yong-zhou Hu

doi:10.3785/j.issn.1008-9292.2003.04.022

[Improved method of epalrestat synthesis]

Zhejiang Da Xue Xue Bao Yi Xue Ban. 2003 Aug;32(4):356-8. doi: 10.3785/j.issn.1008-9292.2003.04.022.

[Article in Chinese]

Authors

Rong Sheng¹, Tao Liu, Yong-zhou Hu

Affiliation

¹ Institute of Pharmaceutic Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310031, China.

PMID: 12970944
DOI: 10.3785/j.issn.1008-9292.2003.04.022

Abstract

Objective: To synthesize epalrestat and to improve the method of synthesis.

Methods: Glycine reacted with carbondisulfide,then with ClCH(2)COONa to give 3-carboxymethylrhodanine. PhCHO reacted with CH(3)CH(2)CHO in NaOH/EtOH solution to produce 2-methylcinnamaldehyde.3-carboxymethylrhodanine and 2-methylcinnamaldehyde were treated with NH(3).H(2)O to obtain epalrestat.

Result: The described method was effective in synthesis of Epalrestat and the yield was higher than that of in references.

Conclusion: The results suggest that this method is suitable for industrial production.

Publication types

English Abstract

MeSH terms

Aldehyde Reductase / antagonists & inhibitors*
Enzyme Inhibitors / chemical synthesis*
Rhodanine / analogs & derivatives*
Rhodanine / chemical synthesis*
Thiazolidines

Substances

Enzyme Inhibitors
Thiazolidines
epalrestat
Rhodanine
Aldehyde Reductase