| 摘要 |
PROBLEM TO BE SOLVED: To obtain the subject new compound having a selective and high V1 receptor affinity, and useful as a V1 receptor antagonist of an arginine vasopressin. SOLUTION: This new triazole derivative is a compound of the formula [A-ring is benzene ring or thiophene ring; R1 is H, a halogen, nitro, amino, a lower alkyl or the like; X is a single bond, O-atom or the like; B-ring is an aryl group which is allowed to be substituted by a lower alkyl or phenyl, or a hetero ring which is allowed to be substituted by a lower alkyl; Y is N or CH; R2 is a lower alkyl, a halogen, hydroxy group or the like; R3 is H or a lower alkyl; R4 is a lower alkyl, a lower alkoxy or the like; (m) is 0, 1-3 integer] or its pharmaceutically permissible salt, e.g. 4-(2-methoxyphenyl)-3-(4'- biphenyl)-1,2,4-triazole. The derivative of the formula is obtained by e.g. reacting a corresponding aromatic carboxylic acid chloride directly with an acid hydrazide to form a diacylhydrazine, performing a ring forming reaction in the presence of a dehydrating agent to obtain 1,3,4-oxazole, and then reacting with an aniline derivative without using a solvent.
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