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【结 构 式】 
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【药物名称】Pinacidil, S-1230, P-1134, Pindac 【化学名称】(±)-N'-Cyano-N-4-pyridinyl-N''-(1,2,2-trimethylpropyl)guanidine monohydrate 【CA登记号】85371-64-8, 60560-33-0 (anhydrous) 【 分 子 式 】C13H21N5O 【 分 子 量 】263.34522 |
【开发单位】Leo (Originator) 【药理作用】CARDIOVASCULAR DRUGS, Hypertension, Treatment of, K(ATP) Channel Activators |
合成路线1
This compound can be obtained in two related ways: 1) By reaction of N-(4-pyridyl)-N'-(1,2,2-trimethylpropyl)thiourea (I) with cyanamide (II) by means of dicyclohexylcarbodiimide (DCC) and ethyldiisopropylamine in ether. 2) The reaction of (I) with phosgene in toluene - THF by means of ethyldiisopropylamine in THF gives N-(4-pyridyl)-N'-(1,2,2-trimethylpropyl)carbodiimide (III), which is condensed with (II) by means of ethyldiisopropylamine.
| 【1】 Petersen, H.J. (Leo Pharmaceutical Products Ltd. A/S); Antihypertensive pyridylguanidine compounds. DE 2557438; FR 2294703; GB 1489879; JP 51086474; US 4057636 . |
| 【2】 Blancafort, P.; Castaner, J.; Serradell, M.N.; Hopkins, S.J.; P-1134. Drugs Fut 1981, 6, 3, 149. |
| 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) | 32176 | N-(4-pyridyl)-N'-(1,2,2-trimethylpropyl)thiourea; N-(4-pyridinyl)-N'-(1,2,2-trimethylpropyl)thiourea | C12H19N3S | 详情 | 详情 | |
| (II) | 19648 | Cyanamide | 420-04-2 | CH2N2 | 详情 | 详情 |
| (III) | 32177 | N-(4-pyridinyl)-N'-(1,2,2-trimethylpropyl)carbodiimide; N-(4-pyridyl)-N'-(1,2,2-trimethylpropyl)carbodiimide | C12H17N3 | 详情 | 详情 |