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【结 构 式】 
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【药物名称】RGH-1756 【化学名称】6-[4-[4-[4-(2-Methoxyphenyl)piperazin-1-yl]butoxy]phenyl]imidazo[2,1-b]thiazole 【CA登记号】207277-37-0 【 分 子 式 】C26H30N4O2S 【 分 子 量 】462.6186 |
【开发单位】Gedeon Richter (Originator) 【药理作用】Antipsychotic Drugs, PSYCHOPHARMACOLOGIC DRUGS, Dopamine D3 Antagonists |
合成路线1
By condensation of 1-(2-methoxyphenyl)piperazine (I) with 6-[4-(4-chlorobutoxy)phenyl]imidazo[1,2-b]thiazole (II) by means of Na2CO3/NaI in refluxing methyl isobutyl ketone.
| 【1】 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) | 11882 | 1-(2-Methoxyphenyl)piperazine; Methyl 2-piperazinophenyl ether; 1-(2-Methoxyphenyl)-piperazine | 35386-24-4 | C11H16N2O | 详情 | 详情 |
| (II) | 20779 | 6-[4-(4-chlorobutoxy)phenyl]imidazo[2,1-b][1,3]thiazole; 4-chlorobutyl 4-imidazo[2,1-b][1,3]thiazol-6-ylphenyl ether | C15H15ClN2OS | 详情 | 详情 |
合成路线2
By meBy methylation of the phenolic precursor (I) with 11C labeled methyl triflate and NaOH in acetone. thylation of the phenolic precursor (I) with 11C labeled methyl triflate and NaOH in acetone.
Extended Information