| 摘要 |
PROBLEM TO BE SOLVED: To obtain a new compound as an intermediate for producing an amidino group-substituted aromatic compound having excellent water solubility and a potent anticoagulant action by peculiarly and reversibly and intensely inhibiting activated blood coagulation factor X even in case of oral administration. SOLUTION: This new compound is 7-methyl-2-naphthalenecarboxamide of formula I. The compound is obtained by adding concentrated ammonia water under cooling to a residue obtained by concentrating solidification of a reaction solution obtained by heating 7-methyl-2-naphthalenecarboxylic acid and thionyl chloride under heating and reflux, stirring the mixture at room temperature, extracting the product using ethyl acetate, washing the extract with water and saturated saline solution, drying, and then distilling away the solvent. The compound is useful as an intermediate for producing a compound of formula II [R1 is carboxyl, an alkoxycarbonyl (methyl) or carboxymethyl; R2 and R3 are each H or a (substituted) 1-6C alkyl; (m) and (n) are each 0-3; and X and Y are each O, S, ethenyl, or the like] as a prophylactic or therapeutic agent for various diseases due to thrombus and embolus. |
