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.
A compound of formula I {R1 is H, OH or a lower alkoxy; Y is a single bond or O; R2 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°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.
UCHIDA MASAHIKO
KIKUCHI NORIHIKO
IZAWA HIDETOSHI
HARA KIYOTO
HONMA TOSHIKI