| 摘要 |
PROBLEM TO BE SOLVED: To obtain the subject new compound comprising a specific indoline compound and having excellent inhibitory actions on activated blood coagulation factor X and useful as a therapeutic or a prophylactic agent for blood coagulating diseases. SOLUTION: This compound is represented by formula I (R1 is H, a 1-6C alkyl or the like; R2 is a 3-10C cycloalkyl or the like; R3 and R4 are each H, a halogen or the like; A is a single bond a 1-4C alkylene or the like; n is 1 or 2), e.g. 2-(7-amidinonaphthalen-2-yl)-1-ethanesulfonyl-5-(piperidin-3-yloxy)ind oline dihydrochloride. The compound represented by formula I is obtained by reacting a compound represented by formula II with alcohols in the presence of an acid (e.g. hydrogen chloride) in an inert solvent (e.g. dichloromethane), preferably at 0-50 deg.C for 1-15 h, providing an iminoether compound and then carrying out an ammonolysis of the resultant iminoether compound in the presence of ammonium ion in an inert solvent at pH 7-9, preferably at 0-50 deg.C for 1-15 h.
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