New type of 5-fluorobenzimidazole derivatives was synthesized through the reaction of 4-fluoro-5-(2,6-dimethylmorpholinyl)-2-aminoaniline with 5-nitro-2-furoic acid and 5-methoxy-3-chlorobenzothiophene-2-carboxylic acid in presence of PPA and treatment of OH-. the resulting substituted 5-fluorobenzimidazole derivatives(6), (7) was characterized by high solubility in common polar organic solvents. We considered 5-fluorobenzimidazole derivatives were useful especially for antifungal drugs. These results are discussed from the viewpoints of the chemical and physical structures of the 5-fluorobenzimidazole derivatives.

[1,2,4]-Triazole derivatives were synthesized by 5 steps. Benzimidazole was refluxed with ethyl chloroacetate to give 1H-benzimidazole-acetic acid ethyl ester (1) over 52% yield. Ester (1) was refluxed with hydrazine hydrate in the presence of ethanol to afford 1H-benzimidazole-1-acetic acid, hydrazide (2). 5-Benzoimidazol-1-ylmethyl-4H-[1,2,4]triazole-3-thiol (4) was made via coupling of compound (2) with methyl isothiocyanate, followed by cyclization of 1H-benzimidazole-1-acetic acid, 2-[(methylamino) thioxomethyl]hydrazide (3) on reflux, and finally the target compounds (6a-6v) were synthesized by general substitution reaction. Compounds (6a-6v) were screened for T-type calcium channel blocker using the fluorescence assay by FDSS6000. All compounds (6a-6v) did not show better activities than control compound, mibefradil.