IMIDAZOLE DERIVATIVE AND THROMBOXANE A2 SYNTHETASE INHIBITOR CONTAINING SAME

摘要

NEW MATERIAL:The compound of formula I (R1 and R2 are H or CH3; when R1 is H, R2 is also H; the double bond in the parentheses m has trans configuration; m is 1 or 2; n is 2-5). EXAMPLE:1-(3-Methoxy-4-hydroxyphenyl)-5-(imidazol-1-yl)-1-penten-3-one. USE:A medicine. A thromboxane A2-synthesis inhibitor. It has strong effect to suppress the coagulation of platelet, contraction of vessel and contraction of bronchus and is effective for the prevention of stenocardia, myocardial infarction, cerebral infarction, bronchial asthma, etc. It is also expected as an agent for preventing metastasis of cancer because the coagulation of platelet participates in the metastasis of cancer. PREPARATION:The compound of formula I can be produced by reacting the aldehyde derivative of formula (R3 and R4 are CH3 or methoxymethyl; k is number of double bonds having trans configuration and is 0 or 1; when R3 is methoxymethyl, R4 is also methoxymethyl) with a phosphonate derivative of formula III (l is 2-5) in the presence of NaH.