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【结 构 式】 
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【药物名称】Bezafibrate, BM-15075, Befizal, Bezalip Retard, Cedur, Bezatol, Bezalip 【化学名称】2-[4-[2-(4-Chlorobenzamido)ethyl]phenoxy]-2-methylpropionic acid 【CA登记号】41859-67-0 【 分 子 式 】C19H20ClNO4 【 分 子 量 】361.82855 |
【开发单位】Norwich Eaton (Originator), Roche (Originator), Kissei (Licensee) 【药理作用】Anti-Hepatitis C Virus Drugs, Anti-Hepatitis Virus Drugs, ANTIINFECTIVE THERAPY, Antiviral Drugs, GASTROINTESTINAL DRUGS, Lipoprotein Disorders, Treatment of , Liver and Biliary Tract Disorders, Treatment of, METABOLIC DRUGS, Drugs Acting on Peroxisome Proliferator-Activated Receptors (PPAR), Fibrates |
合成路线1
The benzoylation of tyramine (2-(p-hydroxyphenyl)ethylamine) (I) with 4-chlorobenzoyl chloride (II) in pyridine gives 4-(4-chlorobenzoylaminoethyl)phenol (III), which by condensation with ethyl alpha-bromoisobutyrate (IV) by means of K2CO3 in refluxing butanone affords ethyl alpha-[4-(4-chlorobenzoylaminoethyl)phenoxy]isobutyrate (V). Finally, this compound is hydrolyzed with KOH in dioxane - water.
| 【1】 Castañer, J.; Thorpe. P.; Bezafibrate. Drugs Fut 1978, 3, 4, 258. |
| 【2】 Witte, E.C.; et al. (Boehringer Ingelheim GmbH); Phenoxyalkylcarbosaurederivate und Verfahren zur Herstellung derselben. DE 2149070; ZA 7206638 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 10295 | p-Chlorobenzoyl chloride; 4-Chlorobenzoyl chloride | 122-01-0 | C7H4Cl2O | 详情 | 详情 |
| (II) | 19988 | 4-(2-Aminoethyl)phenol; Tyramine | 51-67-2 | C8H11NO | 详情 | 详情 |
| (III) | 39798 | 4-chloro-N-(4-hydroxyphenethyl)benzamide | 41859-57-8 | C15H14ClNO2 | 详情 | 详情 |
| (IV) | 39799 | ethyl 2-bromo-2-methylpropanoate | 600-00-0 | C6H11BrO2 | 详情 | 详情 |
| (V) | 39800 | ethyl 2-(4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy)-2-methylpropanoate | C21H24ClNO4 | 详情 | 详情 |