Process optimization and eco-friendly/greener synthesis of some n-aryl/heteryl acetoacetamides

International Current Pharmaceutical Journal Pub Date : 2013-10-08 DOI:10.3329/ICPJ.V2I11.16533

K. Sirisha, I. Rajyalaxmi, S. Olivia

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引用次数: 1

Abstract

N-aryl/heteryl acetoacetamides are the intermediates used in the synthesis of various heterocyclic compounds like 1,4-dihydropyridines, pyrimidines etc. Three different substituted N-aryl/heteryl acetoacetamide derivatives (I-III) have been prepared from the reaction of ethylacetoacetate and three different aryl/heteryl primary amines under solvent free conditions using potassium tert- butoxide as catalyst. The reactions were carried out by two different methods ( viz. , Conventional and Microwave irradiation) and they are simple, eco-friendly and economical. All reactions were processed for optimization with different ratios of aryl/heteryl amine and ethylacetoacetate like1:1,1:1.2,1:1.4,1:1.6,1:1.8,1:2 and a comparison was made between the percentage yields with each ratio. Highest percentage yield was observed with 1:1.8 ratio for I & II and 1:1.6 ratio for III in both the methods. However, the microwave irradiation method was found to be superior to the conventional method. The newly synthesized compounds have been purified by recrystallization and characterized by physical and spectral data. DOI: http://dx.doi.org/10.3329/icpj.v2i11.16533 International Current Pharmaceutical Journal, October 2013, 2(11): 189-192

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一些n-芳基/杂基乙酰乙酰胺的工艺优化及环保合成

n -芳基/杂基乙酰乙酰胺是合成各种杂环化合物如1,4-二氢吡啶、嘧啶等的中间体。以乙酸乙酯和三种不同的芳基/杂基伯胺为原料，叔丁醇钾为催化剂，在无溶剂条件下合成了三种不同取代的n -芳基/杂基乙酰乙酰胺衍生物(I-III)。该反应通过两种不同的方法(即常规和微波辐照)进行，它们简单，环保和经济。以芳杂胺与乙酰乙酸乙酯的比例为1:1、1:1.2、1:1.4、1:1.6、1:1.8、1:2进行优化反应，并比较各比例下的产率。两种方法中，I和II的比例为1:8 . 0,III的比例为1:6 .6，产率最高。然而，微波辐照法被发现优于传统的方法。对新合成的化合物进行了重结晶纯化，并用物理和光谱数据对其进行了表征。DOI: http://dx.doi.org/10.3329/icpj.v2i11.16533国际现代医药杂志，2013年10月，2(11):189-192

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International Current Pharmaceutical Journal

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