公开(公告)号：KR1020000020792A

公开(公告)日：2000-04-15

申请号：KR1019980039546

申请日：1998-09-24

Applicant: 동화약품주식회사

Inventor： 윤성준 ,  이상욱 ,  심형수 ,  박용균 ,  양왕용 ,  김종우 ,  윤제인 ,  이진

IPC: C07D401/14

Abstract: PURPOSE: Title derivatives are provided which has an inhibition effect against HBV(Hepatitis B Virus) and HIV(Human Immunodeficiency Virus) growth. CONSTITUTION: Nicotinic derivatives(formula 2; R4 is H or C1-C4 straight chain or branched alkyl group) and amine compound(formula 3; R1 is C1-C4 straight chain or branched alkoxy or amino group; R2 is H, C1-C4 straight chain or branched alkyl, C1-C3 straight chain or branched hydroxy alkyl, C2-C4 alkyl thioalkyl, phenyl, benzyl or hydroxy benzyl group; R3 is H or methyl group; n is 0-1) are reacted to give the derivatives(formula 1). Thus, 2 g of 6-£1-£3-isopropyl amino)-2-pyridyl|piperazin-4-yl-carbonyl|nicotine acid and 0.8 ml of triethyl amine are dissolved in 30 ml of methylene chloride, and slowly added 0.7 ml of pivaloyl chloride at 0- 5°C. Reactant is reacted at 5°C for 1 hour, followed by addition of 2.5 ml of N,N-diisopropyl ethyl amine and 0.83 g of glycine ethyl ester at 10°C for 2 hour to give 1.89 g of N-(ethoxycarbonyl methyl)-6-£1-£3-isopropyl amino)-2-pyridyl|piperazin-4-yl-carbonyl|nicotine amide hydrochloride.

Abstract translation: 目的：提供对HBV（乙型肝炎病毒）和HIV（人类免疫缺陷病毒）生长具有抑制作用的标题衍生物。 构型：烟碱衍生物（式2; R4为H或C1-C4直链或支链烷基）和胺化合物（式3; R1为C1-C4直链或支链烷氧基或氨基; R2为H，C1-C4 直链或支链烷基，C1-C3直链或支链羟基烷基，C2-C4烷基硫代烷基，苯基，苄基或羟基苄基; R3是H或甲基; n为0-1）反应，得到衍生物 公式1）。 因此，将2g 6- {1- {3-异丙基氨基）-2-吡啶基|哌嗪-4-基羰基|尼古丁酸和0.8ml三乙胺溶于30ml二氯甲烷中，并缓慢加入0.7 ml的新戊酰氯在0-5℃。 反应物在5℃下反应1小时，然后在10℃下加入2.5ml N，N-二异丙基乙基胺和0.83g甘氨酸乙酯2小时，得到1.89g N-（乙氧基羰基甲基） -6- {1- {3-异丙基氨基} -2-吡啶基}哌嗪-4-基 - 羰基}烟碱酰胺盐酸盐。