| 摘要 |
PURPOSE: To obtain the subject pharmaceutical agent having inhibiting effect on calcium uptake of leukocytes and platelets and useful for treating rheumatoid arthritis, neutrophilic dermatitis, myocardial infarction, etc., by compounding a new 1-phenyl-3-aryl-2-propyn-1-one. CONSTITUTION: Trimethylsilylacetylene is made to react with a benzaldehyde compound of formula I (R1 to R3 are each H, a 1-6C alkyl, a 1-6C alkoxy, a halogen, etc.) in the presence of a base to produceα-[(trimethylsilyl) ethyl]benzenemethanol compound. Then, the trimethylsilyl group is removed from the obtained compound to produce anα-(ethynyl)benzenemethanol compound of formula II. The product is made to react with an aryl halide of the formula: ArX (Ar is a group of formula III, formula IV, etc.; X is a halogen) followed by oxidation. Thus, a 1-phenyl-3-aryl-2-propyn-1-one compound of formula V is obtained. Subsequently, formulation is carried out using the compound as an active ingredient to obtain the objective pharmaceutical preparation having inhibiting effect on calcium uptake of leukocytes and platelets.
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