| 摘要 |
NEW MATERIAL:A compound expressed by formula I (X is O or methylene; n is 2-4). EXAMPLE:Ethyl 4-(5-fluorobenzothiazol-2-yl)benzyl-2-oxopyrrolidinophosphinate. USE:A preventive agent and remedy for ischemic cardiopathy, e.g. angina pectoris, myocardial infarction, arrhythmia, etc. having calcium antagonistic actin. PREPARATION:Diethyl 4-(5-fluorobenzothiazol-2-yl)benzylphosphonate expressed by formula III is refluxed in the presence of excess thionyl chloride and preferably a catalytic amount of dimethylformamide (DMF) normally for 2-4hr to give phosphonyl chloride hydrochloride expressed by formula III, which is reacted with a compound expressed by formula IV in a molar amount of 1-3 times based on the compound expressed by formula III in the presence of an organic amine, e.g. triethylamine, in a reaction solvent at 0 deg.C-room temperature for 1-24hr.
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