-
1.
公开(公告)号:KR100476359B1
公开(公告)日:2005-03-16
申请号:KR1020010052436
申请日:2001-08-29
Applicant: 주식회사한국신약
IPC: C07D209/24
Abstract: 본 발명은 하기 화학식 1로 표시되는 지질 과산화 저해제로 유용한 벤자스타틴 유도체의 기본 골격 구조를 갖는 화합물 및 그의 제조방법에 관한 것으로, 보다 구체적으로 본 발명의 화합물은 지질 과산화 억제 활성이 우수한 벤자스타틴 유도체 및 그의 유도체를 제조하는데 유용한 중간체로 사용할 수 있다.
(상기식에서, R
1 ,
R
2 및
R
3 는 명세서 내에 기재된 바와 같다.)-
公开(公告)号:KR1020020018100A
公开(公告)日:2002-03-07
申请号:KR1020010052436
申请日:2001-08-29
Applicant: 주식회사한국신약
IPC: C07D209/24
Abstract: PURPOSE: Provided is a novel compound useful as an intermediate in manufacturing benzastatin derivatives having an excellent inhibition activity of lipid peroxidation. Also, its manufacturing method is provided. CONSTITUTION: The novel compound is a basic structure of benzastatin useful as an inhibitor of lipid peroxidation and represented by the formula(1), wherein R1 is H, CH3, OH, nitrile group, amide group, C1-C4 alkoxy group or hydroxymethyl group; R2 is a nitrogen protection group, such as H, CH3 or PMB(paramethoxy benzyl); and R3 is H, CH3, C1-C10 alkyl group or partially unsaturated linear or branched hydrocarbon. Aldehyde compound of the formula(1a) is manufactured by the steps of: reducing a compound of the formula(5) with a reductant to prepare a compound of the formula(6); and oxidizing the alcohol compound of the formula(6) to obtain a compound of the formula(1a).
Abstract translation: 目的:提供一种在制备具有优异的脂质过氧化抑制活性的苯达斯汀衍生物中作为中间体的新型化合物。 此外,还提供了其制造方法。 构成:新化合物是用作脂质过氧化抑制剂的苯达斯汀的基本结构,由式(1)表示,其中R1是H,CH3,OH,腈基,酰胺基,C1-C4烷氧基或羟甲基 ; R2是氮保护基团,例如H,CH 3或PMB(对甲氧基苄基); 并且R 3是H,CH 3,C 1 -C 10烷基或部分不饱和直链或支链烃。 通过以下步骤制备式(1a)的醛化合物:用还原剂还原式(5)的化合物以制备式(6)的化合物; 氧化式(6)的醇化合物,得到式(1a)的化合物。
-