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Title:
3-AMIDINOPHENYL ETHER DERIVATIVE, ACTIVATED BLOOD COAGULATION FACTOR X INHIBITOR AND INTERMEDIATE FOR PRODUCING THE SAME
Document Type and Number:
Japanese Patent JPH11140040
Kind Code:
A
Abstract:

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.


Inventors:
AKAHA SATOSHI
UCHIDA MASAHIKO
KIKUCHI NORIHIKO
IZAWA HIDETOSHI
HARA KIYOTO
HONMA TOSHIKI
Application Number:
JP34183997A
Publication Date:
May 25, 1999
Filing Date:
November 06, 1997
Export Citation:
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Assignee:
KISSEI PHARMACEUTICAL
International Classes:
C07D211/46; A61K31/165; A61K31/40; A61K31/435; A61K31/445; A61K31/4465; A61K31/451; A61P7/02; A61P43/00; C07C255/54; C07C257/18; C07D207/12; (IPC1-7): C07C257/18; A61K31/165; A61K31/40; A61K31/435; A61K31/445; C07C255/54; C07D207/12; C07D211/46