Vasincu Ioana, Apotrosoaei Maria, Panzariu Andreea, Buron F, Routier S, Profire Lenuta
Rev Med Chir Soc Med Nat Iasi. 2014 Jan-Mar;118(1):219-24.
Ibuprofen, an important nonsteroidal anti-inflammatory agent, is one of the most prescribed drugs for the treatment of pain and inflammation from various rheumatic diseases, but some side effects can occur on long-term use.
The method for synthesis optimization of new derivatives of Ibuprofen with thiazolidin-4-one moiety, with improved pharmacological and toxicological profile.
To optimize the derivatization method of free carboxyl group of Ibuprofen (2-(4-isobutylphenyl)propionic acid) the reaction conditions were varied (reagent ratio, catalyst, reaction medium).
The most favorable method was proved to be the reaction between ibuprofen hydrazone and mercaptoacetic acid, in excess, at 80-85 degrees C, for 6 h with 96% conversion rate.
The synthesis of 2-phenyl-3-[2-(4-(isobutyl)phenyl)-2-methyl]acetamido-thiazolidin-4-one derivative was optimized in view of applying it as a general procedure for the synthesis of other derivatives with related structure. The chemical structure and molecular weight of the synthesized compound were confirmed by spectral methods (IR, 1H NMR, 13C NMR, HR-MS).
布洛芬是一种重要的非甾体抗炎药，是治疗各种风湿性疾病疼痛和炎症最常用的处方药之一，但长期使用可能会出现一些副作用。
优化具有噻唑烷-4-酮部分的布洛芬新衍生物的合成方法，以改善其药理和毒理学特性。
为优化布洛芬（2-(4-异丁基苯基)丙酸）游离羧基的衍生化方法，改变反应条件（试剂比例、催化剂、反应介质）。
最有利的方法是异丁苯丙酸腙与过量巯基乙酸在80 - 85℃反应6小时，转化率为96%。
鉴于将其作为合成其他相关结构衍生物的通用方法，对2-苯基-3-[2-(4-(异丁基)苯基)-2-甲基]乙酰胺基-噻唑烷-4-酮衍生物的合成进行了优化。通过光谱方法（红外光谱、1H核磁共振、13C核磁共振、高分辨质谱）确认了合成化合物的化学结构和分子量。
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