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Activated hydrotalcites as catalysts for the synthesis of chalcones of pharmaceutical interest

机译:活化的水滑石作为催化剂合成具有药用价值的查耳酮

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The Claisen-Schmidt condensation between benzaldehyde and acetophenone has been carried out in the presence of calcined-rehydrated hydrotalcites a solid-base catalysts.The rehydration method can the effect of the water content as well as the chemical composition of the rehydrated Al-Mg mixed oxides have been studied.The results showed that an Al-Mg mixed oxide with an Al/(Al+Mg) molar ratio of 0.25 with a water content of 35at% was the optimum catalysts which gives excellent activity for this type of condensation.This optimized achieving has been applied to the synthesis of several chalcones with antiinflammatory,antineoplastic,and diuretic pharmacological activities achieving in all cases excellent activity and selectivity to the corresponding chalcones.A comparative study in the homogeneous phase using KOH as base catalyst showed that the rehydrated Al-Mg mixed oxides can compete with the conventional KOH when the reaction is performed at higher reaction temperatures.This behavior is not attributed to a lower intrinsic activity of the active sites on the solid,but to the small concentration of accessible active sitex existing on the rehydrated sample.
机译:苯甲醛和苯乙酮之间的Claisen-Schmidt缩合反应是在煅烧的再水合水滑石粉作为固体碱催化剂存在下进行的。再水化方法可以影响水含量以及再水合的Al-Mg混合物的化学组成结果表明,Al /(Al + Mg)摩尔比为0.25,水含量为35at%的Al-Mg混合氧化物是最佳的催化剂,对这类缩合反应具有出色的活性。优化的实现已应用于合成具有抗炎,抗肿瘤和利尿药理活性的查尔酮,在所有情况下均对相应的查尔酮具有优异的活性和选择性。以KOH为基础催化剂的均相比较研究表明,再水合的Al在较高的反应温度下进行反应时,-Mg混合氧化物可以与常规KOH竞争。并不是由于固体上活性位点的固有活性较低,而是归因于复水样品上存在的活性位点浓度低。

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