3-AMIDINOPHENYL ETHER DERIVATIVE, ACTIVATED BLOOD COAGULATION FACTOR X INHIBITOR AND INTERMEDIATE FOR PRODUCING THE SAME
PROBLEM TO BE SOLVED: To provide the subject new compound having an excellent activity for inhibiting the activated blood coagulation factor X and useful as an activat ed blood coagulation factor X inhibitor. SOLUTION: A compound of formula I R is H, OH or a lower alkoxy; Y is a single bond or O; R...
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Zusammenfassung: | PROBLEM TO BE SOLVED: To provide the subject new compound having an excellent activity for inhibiting the activated blood coagulation factor X and useful as an activat ed blood coagulation factor X inhibitor. SOLUTION: A compound of formula I R is H, OH or a lower alkoxy; Y is a single bond or O; R is a lower alkyl or a group of formula II [(n) is 1 or 2; T is H or a group of the formula: C(=NH)-W (W is a lower alkyl]}, for example, N-[2-(3-amidinophenyoxy)ethyl]-4-isopropylbenzamide hydrochloride. The compound of formula I is obtained by allowing a 3-cyanophenyl ether derivative of formula III or its salt to react with an alcohol in the presence of a hydrogen halide such as hydrogen chloride at -20 deg.C to room temperature and subsequently allowing the obtained imidate compound to react with ammonia or an ammonium salt such as ammonium carbonate. The solvent used therein includes methanol and ethanol. |
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