| Summary: | 碩士 === 中國醫藥學院 === 藥物化學研究所 === 88 === Abstracts
The key intermediate, 2-(4-ethoxycarbonyphenyl)benzimidazole (1) was prepared by condensation of 1,2-phenylenediamine with methyl 4-formylbenzoate, in the presence of cupric acetate. When compound 1 was reacted with benzyl chloride and K2CO3 in alcohol, the designed product, 1-benzyl—2-(4-ethoxycarbonylphenyl)benzimidazole (3) with unexpected product, 2-benzylamino-N-benzyl-N-(4-ethoxycarbonylphenylcarbonyl)-aniline (4) were obtained. Compound 1 was then allowed to react with a variety of halo benzyl chlorides to affored the corresponding 1-halobenzyl-2-(4-ethoxy-carbonylphenyl)benzimidazole (5, 7, 9, 11, 13, 15) and 2-halobenzylamino-N-halobenzyl-N-(4-ethoxycarbonylphenylcarbonyl)aniline (6, 8, 10, 12, 14, 16).
The antiplatelet activity of lead compound (3) exhibibited significant inhibitory effect against AA- and collagen-induced platelet aggregation; whereas unlike YD-3, it demonstrated no inhibitory effect against thrombin-induced platelet aggregation at does up to 100μg/ml. Screening tests of antiplatelet activities of other synthesized compounds 1, 2 and 4-24 are in progress and will be reported later.
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