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【结 构 式】 
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【药物名称】CP-060 【化学名称】3-[3-[N-[2-(1,3-Benzodioxol-5-yloxy)ethyl]-N-methylamino]propyl]-2-(3,5-di-tert-butyl-4-hydroxyphenyl)thiazolidin-4-one 【CA登记号】 【 分 子 式 】C30H42N2O5S 【 分 子 量 】542.74364 |
【开发单位】Chugai (Originator) 【药理作用】CARDIOVASCULAR DRUGS, Hypertension, Treatment of, Calcium Channel Blockers, Lipid Peroxidation Inhibitors |
合成路线1
Aldehyde (I) was condensed with 3-aminopropanol (II) in refluxing benzene using a Dean-Stark trap to give imine (III) which, without purification, was in turn condensed with a-mercaptoacetic acid (IV) to afford thiazolidinone (V). Treatment of alcohol (V) with PBr3 gave bromide (VI). Then, reaction of (VI) with amine (VII) in the presence of K2CO3 in refluxing acetone produced the target compound.
| 【1】 Kato, T.; Ozaki, T.; Tamura, K.; Suzuki, Y.; Akima, M.; Ohi, N.; Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 1. 2-(3,5-Di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones. J Med Chem 1998, 41, 22, 4309. |
| 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) | 14875 | 3,5-Bis(1,1-dimethylethyl)-4-hydroxybenzaldehyde; 3,5-di(tert-butyl)-4-hydroxybenzaldehyde; 3,5-Di-tert-butyl-4-hydroxybenzaldehyde | 1620-98-0 | C15H22O2 | 详情 | 详情 |
| (II) | 18522 | 3-amino-1-propanol | 156-87-6 | C3H9NO | 详情 | 详情 |
| (III) | 18523 | 2,6-di(tert-butyl)-4-[[(3-hydroxypropyl)imino]methyl]phenol | C18H29NO2 | 详情 | 详情 | |
| (IV) | 18524 | 2-sulfanylacetic acid | 68-11-1 | C2H4O2S | 详情 | 详情 |
| (V) | 18525 | 2-[3,5-di(tert-butyl)-4-hydroxyphenyl]-3-(3-hydroxypropyl)-1,3-thiazolidin-4-one | C20H31NO3S | 详情 | 详情 | |
| (VI) | 18526 | 3-(3-bromopropyl)-2-[3,5-di(tert-butyl)-4-hydroxyphenyl]-1,3-thiazolidin-4-one | C20H30BrNO2S | 详情 | 详情 | |
| (VIII) | 12561 | 2-(1,3-Benzodioxol-5-yloxy)-N-methyl-1-ethanamine; N-[2-(1,3-Benzodioxol-5-yloxy)ethyl]-N-methylamine | C10H13NO3 | 详情 | 详情 |
Extended Information