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【结 构 式】 
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【药物名称】RP-66681 【化学名称】(+)-N-[3-[alpha-[(Z)-1-Methyl-4-piperidinyloxyimino]benzyl]phenyl]-3alpha-(3-pyridyl)-1H,3H-pyrrolo[1,2-c]thiazole-7-carboxamide 【CA登记号】132710-24-8 【 分 子 式 】C31H31N5O2S 【 分 子 量 】537.68902 |
【开发单位】Aventis Pharma (Originator) 【药理作用】Platelet-Activating Factor (PAF) Antagonists |
合成路线1
This compound has been obtained by two similar ways: 1. By condensation of the benzophenone derivative (I) with O-(1-methylpiperidin-4-yl)hydroxylamine by means of K2CO3 in propanol. 2. The reaction of benzophenone derivative (I) with hydroxylamine by means of K2CO3 in propanol gives the corresponding oxime (III), which is finally alkylated with 4-chloro-1-methylpiperidine (IV) by means of NaH in DMF.
| 【1】 Floch, A.; Soler, F.; Cavero, I.; Lavé, D.; Robaut, C.; RP 66681B, a water-soluble pyrrolothiazole derivative with potent and selective PAF receptor antagonist properties. Drugs Fut 1992, 17, 3, 207. |
| 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) | 43196 | (3S)-N-(3-benzoylphenyl)-3-(3-pyridinyl)-1H-pyrrolo[1,2-c][1,3]thiazole-7-carboxamide | C25H19N3O2S | 详情 | 详情 | |
| (II) | 43197 | O-(1-methyl-4-piperidinyl)hydroxylamine; 4-(aminooxy)-1-methylpiperidine | C6H14N2O | 详情 | 详情 | |
| (III) | 43198 | (3S)-N-[3-[(hydroxyimino)(phenyl)methyl]phenyl]-3-(3-pyridinyl)-1H-pyrrolo[1,2-c][1,3]thiazole-7-carboxamide | C25H20N4O2S | 详情 | 详情 | |
| (IV) | 20949 | 4-Chloro-1-methylpiperidine; 4-Chloro-N-methylpiperidine; N-methyl-4-chloropiperidine | 55770-77-4 | C6H12ClN | 详情 | 详情 |
Extended Information