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US 2021/0061772 A1Published application
Method for preparing tolimidone on large scale
AssigneeBukwang Pharmaceutical Co., Ltd.
InventorsKwang Ok LEE, Kyung Hwa LEE, Eun Ju JEONG
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Abstract
The present disclosure relates to a method for preparing tolimidone on large scale with maintaining high purity and uniform particle size distribution, and more specifically, a method suitable for preparing tolimidone on industrially large scale by using tetrabutyl ammonium bromide catalyst and recrystallization in ethanol, which can prepare highly pure tolimidone in a time shorter than prior arts while maintaining water content and particle size distribution constantly.
Claims14
A method for preparing tolimidone, comprising:
- (i) reacting the compound of formula 6 and the compound of formula 5 in the presence of a tetra-substituted ammonium salt catalyst to prepare the compound of formula 4;
- (ii) conducting Vilsmeir reaction for the prepared compound of formula 4 to prepare the compound of formula 3;
- (iii) refluxing with agitation the prepared compound of formula 3 together with urea and an alkoxide base to prepare the salt compound of formula 2;
- and
- (iv) desalting the prepared salt compound of formula 2 to obtain tolimidone of formula 1 and recrystallizing the obtained tolimidone with an alcohol that corresponds to the alkoxide base:
- wherein A+ is a cation of the alkoxide base.
3 more elements
Dependencies are inferred from the claim text.