公开(公告)号：KR1020000031735A

公开(公告)日：2000-06-05

申请号：KR1019980047918

申请日：1998-11-10

Applicant: 동화약품주식회사

Inventor： 윤성준 ,  이상욱 ,  심형수 ,  박용균 ,  양왕용 ,  김종우 ,  박상진

IPC: C07D401/14

Abstract: PURPOSE: 2,5-pyrimidinedicarboxylic acids and the method for manufacturing it are provided, which have effect on restraining the proliferation of HBV(Hepatitis B Virus) and HIV(Human Immunodeficiency Virus). CONSTITUTION: In the formula 1, R1 represents hydrogen, alkyl group, hydroxy alkyl group, alkoxy alkyl group, dihydroxy alkyl group and dialkoxy alkyl group and R2 represents hydrogen and alkyl group. 2,5-pyridinedicarboxylic acids(formula 1) can form organic or inorganic salt such as chloric acid, phosphoric acid, oxalic acid, maleic acid and tartaric acid which is admitted pharmaceutically. 2,5-pyridinedicarboxylic acids are prepared from following reaction(reaction 1). Piperazines are piperazine(R1=hydrogen), 1-methylpiperazine(R1=methyl group), 1-ethylpiperazine(R1=ethyl group), 1-(2-hydroxyethyl)piperazine(R1=2-hydroxyethyl group. Nicotinic acids(formula 2) are reacted with acyl chloride, product of this reaction is reacted with piperazine compounds and 2,5-pyrimidinedicarboxylic acids are prepared from this reaction.

Abstract translation: 目的：提供2,5-嘧啶二羧酸及其制备方法，其具有抑制HBV（乙型肝炎病毒）和HIV（人类免疫缺陷病毒）增殖的作用。 构成：在式1中，R 1表示氢，烷基，羟基烷基，烷氧基烷基，二羟基烷基和二烷氧基烷基，R 2表示氢和烷基。 2,5-吡啶二羧酸（式1）可以形成有机或无机盐，例如药学上允许的氯酸，磷酸，草酸，马来酸和酒石酸。 从以下反应制备2,5-吡啶二羧酸（反应1）。 哌嗪是哌嗪（R1 =氢），1-甲基哌嗪（R1 =甲基），1-乙基哌嗪（R1 =乙基），1-（2-羟乙基）哌嗪（R1 = 2-羟乙基）烟酸（式2 ）与酰氯反应，将该反应产物与哌嗪化合物反应，并从该反应制备2,5-嘧啶二羧酸。