|
【结 构 式】 
|
【药物名称】 【化学名称】2-[4-[4-[4-(2-Methoxyphenyl)piperazin-1-yl]butoxy]- phenyl]imidazo[1,2-a]pyridine 【CA登记号】207277-28-9 【 分 子 式 】C28H32N4O2 【 分 子 量 】456.59284 |
【开发单位】Gedeon Richter (Originator) 【药理作用】Antipsychotic Drugs, PSYCHOPHARMACOLOGIC DRUGS, Dopamine D3 Antagonists |
合成路线1
Coupling between phenol derivative (I) and 1-bromo-4-chlorobutane (II) by means of either Na2CO3/NaI or K2CO3 in refluxing 5-methyl-2-hexanone affords 4-chlorobutoxy derivative (III), which is then converted into the desired product by condensation with (2-methoxyphenyl)piperazine dihydrochloride (IV), either by means of Na2CO3/NaI or with K2CO3 in refluxing 5-methyl-2-hexanone.
| 【1】 Laszlovszky, I.; et al.; Substituted phenoxyalkylpiperazines as dopamine D3 receptor ligands. Pharmazie 2001, 56, 4, 287. |
| 【2】 Laszlovszky, I.; Domány, G.; Ferenczy, G.; Szántay, C. Jr.; Thuroczyné Kálmán, E.; Lapis, E.; Trischler, F.; Hegedús, B.; Auth, F.; Csejtei, M.; Kárpáti, E.; Kiss, B.; Laszy, J.; Pellioniszné Paróczai, M.; Sarkadi, A.; Szabó, S. (Gedeon Richter Ltd.); 2-Methoxyphenylpiperazine derivs.. EP 0935599; US 6103724; WO 9818797 . |
| 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) | 50184 | 4-imidazo[1,2-a]pyridin-2-ylphenol | C13H10N2O | 详情 | 详情 | |
| (II) | 16141 | 1-bromo-4-chlorobutane | 6940-78-9 | C4H8BrCl | 详情 | 详情 |
| (III) | 50185 | 2-[4-(4-chlorobutoxy)phenyl]imidazo[1,2-a]pyridine; 4-chlorobutyl 4-imidazo[1,2-a]pyridin-2-ylphenyl ether | C17H17ClN2O | 详情 | 详情 | |
| (IV) | 11882 | 1-(2-Methoxyphenyl)piperazine; Methyl 2-piperazinophenyl ether; 1-(2-Methoxyphenyl)-piperazine | 35386-24-4 | C11H16N2O | 详情 | 详情 |
Extended Information