Synthesis of 4- and 5- nitro-substituted heteroaryl cinnamoyl derivatives

In the condensation of the 4and 5-nitro-substituted 2-acetyl-1,3-indandione with heteroaryl aldehydes in the presence of alkaline or acidic catalysts, the corresponding cinnamoyl derivatives are obtained that possess anticoagulant activity, compared with that of 2-acetyl-1,3-indandione. It has been proven that some of the sodium salts of the cinnamoyl-indandione possess anticoagulant activity. Different derivatives of 2-acyl-1,3indandione manifest as anticoagulant agents and as such they are widely used in medicine and in fighting rodents [1-3]. Certain 2-acyl-1,3-indandiones have impact on Mycobacterium tuberculosis [4-6]. A number of complexes were obtained [7-10]. 2-Acyl1,3-indandiones are prepared from dialkyl phthalate with the corresponding methyl ketones in the presence of CH 3 ONa [11, 12]. Literature reveals a number of examples which show that the replacement of saturated with unsaturated radical very often increases the physiological effect or it is very specific [13, 14].