A one pot highly efficient and simple protocol for the construction of aromatic cyanamides from thioureaviadesulphurization/C–N cross coupling using a cheap, readily available and air stable copper source as a catalyst has been described.
Ad iverses cope of 2-aryl-1,3-dicarbonyl substrates was investigated in an efficient and facile enolate-directed CÀHa lkenylation process using readily availablee lectron-deficient alkenes. The developed domino strategy works under rhodium catalysis, providing ar ange of benzopyran heterocycles by the formationo ft wo distinct CÀCa nd CÀOb onds and one new six-membered ring. The salient features of the protocoli nclude the broad range of previously unexplored 1,3-dicarbonyl substrates for CÀHa lkenylations, good functional group tolerance and rapid assembly of new benzopyrans in generally good to excellent isolated yields. Figure 1. Selected examples of bioactive benzopyrans.[a] Dr.
Preparation of a biologically active benzofuran derivative ethyl 2-(4-fluorophenyl)-5-hydroxy-6-nitrobenzofuran-3-carboxylate from commercially available starting materials 2-bromo-4-methoxy-phenol and parafluorophenylacetylene is described in four steps with good yields. The final compound and all the intermediates reported in the method were characterized by spectroscopic techniques. Finally, the target molecule and its methyl derivative were tested for their anticancer activity and were found to be 95.2 μg/mL and 8.5 μg/mL (IC 50 ) respectively against HCT 116 cell line.
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