The Synthesis And Characterizing Of Novel Benzimidazole Compounds

In this thesis, 32 compounds of three series of benzimidazole compounds have beendesigned and synthesized, among them 22 compounds have not been reported in literature.First, glycosyl has been inducted into the structures of benzimidazole hydrazides,employing benzimidazole and 2-aminobenzimidazole as starting materials, and usingglycosyl isothiocyanates as useful intermediates, two series of glycosides have beendesigned and synthesized. Second, one series of benzimidazole hydrazones have beensynthesized inducting aromatic aldehydes. The new compounds have been characterized bymeans of elemental analysis, IR and ~1HNMR. One novel single crystal of benzimidazolederivatives has been successfully prepared and studied by X-ray diffraction technique. Thecrystal structure is reported precisely, including bond lengths, bond angles, torsion anglesand so on.The contents and the primary contributions of the research are summarized as follows:(1) Several novel aminothiourea compounds bearing benzimidazole and glycosylframeworks have been synthesized utilizing D-glucose, D-galactose, D-xylose, lactose andbenzimidazole as starting materials, respectively. They have been expected to displayvarious bioactivities. The biological activities of new compounds have been tested.(2) Glycosyl isothiocyanates have been synthesized utilizing D-glucose, D-galactose,D-xylose, and as starting materials. Several novel aminothiourea compounds bearing2-aminobenzimidazole and glycosyl frameworks have been synthesized using glycosylisothiocyanates. The induction of life matter may efficiently improve their biologicalactivities against tumor.(3) A series of novel benzimidazole hydrazones bearing -C=N and aromatic group have been synthesized utilizing 2-aminobenzimidazole as starting materials via a five-stepprocedure. They have been preliminarily determined to display biological activity.(4) One novel single crystal of benzimidazole derivatives has been successfullyprepared and studied by X-ray diffraction technique. Their crystal datas are reportedprecisely, including bond lengths, bond angles, torsion angles and so on, so that thestructure and configuration are confirmed. The crystal is: 2-(4-methoxybenzoyl-amino)benzimidazole.(5) The biological activities and thermal stability of some benzimidazole derivativesare discussed.