124782-64-5Relevant articles and documents
Preparation method of epalrestat
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Paragraph 0047-0070, (2021/10/11)
The invention relates to the technical field of medicines, in particular to a preparation method of epalrestat. The preparation method provided by the invention comprises the steps of mixing 3-carboxymethyl rhodanine, alpha-methylcinnamyl aldehyde, a catalyst and water, and sequentially carrying out condensation reaction and acid neutralization to obtain an epalrestat crude product, wherein the catalyst comprises a basic catalyst and a phase transfer catalyst; and mixing the epalrestat crude product with an alcohol organic solvent, and recrystallizing to obtain the epalrestat. The preparation method adopts water as a reaction solvent, and is safe and environment-friendly; the existing three procedures such as crude product preparation, acidification dissociation and recrystallization are simplified into two procedures such as crude product preparation and recrystallization, and the two procedures such as crude product preparation and acidification dissociation are combined into one, so that the procedures are simplified; and an alcohol organic solvent is adopted for recrystallization, so that recycling is facilitated.
PROCESS FOR PREPARING EPALRESTAT
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Paragraph 0058, (2017/08/08)
PROBLEM TO BE SOLVED: To provide processes for preparing and purifying 2-((Z)-5-((E)-2-methyl-3-phenyl-allylidene)-4-oxo-2-thioxo-thiazolidin-3-yl) acetic acid (epalrestat). SOLUTION: Provided are processes for preparing and purifying epalrestat represented by the following formula (I), comprising the steps of: reacting rhodanine-3-acetic acid with (E)-2-methyl-3-phenyl-acryl-aldehyde in the presence of an ammonium salt(s) of an organic acid such as citric acid and DMF-containing solvent(s); isolating the produced epalrestat DMF solvate and drying it; suspending said epalrestat DMF solvate in ethanol; and further isolating the generated epalrestat crystal and drying it. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT