[Improved method of epalrestat synthesis].
To synthesize epalrestat and to improve the method of synthesis.



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.



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



The results suggest that this method is suitable for industrial production.
Sheng
Rong
R
Institute of Pharmaceutic Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310031, China.
Liu
Tao
T
Hu
Yong-zhou
YZ
D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis*; D012236:Rhodanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis*; D053778:Thiazolidines
D004791:Enzyme Inhibitors; D053778:Thiazolidines; C038131:epalrestat; D012236:Rhodanine; D000449:Aldehyde Reductase