A series of isomeric ureide derivatives of novel 2,4-disubstituted pyrimidinopiperidines were synthesized starting from 2,4dichloropyrimidine. All the final products were purified on silica and characterized by spectral analysis. Both the 2,4-disubstituted pyrimidinopiperidines were analyzed for their in vitro anticancer activity on the cell lines HCT116, MIA-PaCa2 and MDA-MB 231 by using MTT cell proliferation assay. Further, the antimicrobial studies were carried out against different bacterial and fungal strains by employing cup plate method. These compounds were showed significant anticancer activity on tested three cancer cell lines and exhibited potent antimicrobial activity in tested strains of bacteria and fungi. Results and Discussion Chemistry Synthesis of ureide derivatives of 2-aryl-4-(-4-amino piperidinyl) pyrimidines (5 a-l):The reaction of 2,4-dichloro-pyrimidine (1) with tert-butylpiperidin-4-ylcarbamate in presence of diisopropylethylamine in dichloromethane at room temperature afforded the 4-substituted 2-chloropyrimidine derivative 2 a with 62% yield (Scheme 1) after purifying by column Scheme 1. Reagents and conditions: i) tert-butyl-piperidin-4yl-carbamate, DIPEA, THF, rt, 4 h; ii) R = a-d, Pd 2 (dba) 3 , X-Phos, DIPEA, rt, 18 h; iii) TFA, DCM, rt, 10 min; iv) R 1 = e-g, DIPEA, reflux, 10 min. EntryAmino piperidine derivative (4 A-4D) Isocyanate (e-g) Urea derivative (5 A-5 L) Yield (%) 6 95 7 92 8 91 9 95 10 92

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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