METHOD FOR MANUFACTURING PYRIMIDINE COMPOUND AND ITS SALT

摘要

PURPOSE: Provided is a method for manufacturing pyrimidine compound and its salt. Particular, pyridine derivatives useful for cardiocirculation diseases are manufactured in a high yield by antagonistic reaction to angiotensin II receptor. CONSTITUTION: The method for manufacturing pyridine compound of the formula(1) and its slat comprises the steps of: thio-amidating a compound of the formula(7) using Lawessons reagent; and treating the reacted compound with alcohol based reagent. In the formulae, R1 is C1-C4 linear or branched alkyl, cyclo alkyl, C1-C4 alkylalkoxy, or C1-C4 alkylmercapto; R2 is hydrogen, halogen, C1-C4 linear or branched alkyl or aryl, or arylalkyl; and R3 and R4 are the same or different each other, and can be one of hydrogen, halogen, hydroxy, C1-C4 alkoxy, amino, alkylamino or dialkylamino(each alkyl residue has 1-5 carbons), C1-C4 alkoxycarbonyl, carboxy, or C1-C4 linear or branched alkyl substituted with substituted aminocarbonyl, cycloalkyl, aryl, arylalkyl, C1-C4 alkyl or arylcarbonyl, C1-C4 alkoxycarbonyl or substituted aminocarbonyl, or form 4-8 membered cyclic ring with nitrogen atoms, wherein the cyclic ring can be substituted with one or two substituent selected from the group consisting of hydrogen, hydroxy, C1-C4 alkoxy, amino, alkylamino or dialkylamino(each alkyl residue has 1-5 membered carbon), C1-C4 alkoxycarbonyl, carboxy, substituted aminocarbonyl, and it can include -O-, -S-, -SO-, -SO2-, N-R5, in which R¬5 is hydrogen, C1-C4 alkyl, aryl, arylalkyl, substituted alkenyl, pyridyl, pyrimidyl, C1-C4 alkyl or arylcarbonyl, C1-C4 alkoxycarbonyl, substituted aminocarbonyl; and n is an integer of 1-6.