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【结 构 式】 
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【药物名称】HA-1004 【化学名称】N-(2-Guanidinoethyl)-5-isoquinolinesulfonamide hydrochloride 【CA登记号】91742-10-8 【 分 子 式 】C12H16ClN5O2S 【 分 子 量 】329.81062 |
【开发单位】Asahi Kasei (Originator), Mie University (Originator) 【药理作用】Angina pectoris, Treatment of, CARDIOVASCULAR DRUGS, Treatment of Disorders of the Coronary Arteries and Atherosclerosis, Calcium Channel Blockers |
合成路线1
The reaction of 5-isoquinolinesulfonyl chloride (I) with ethyldiamine (II) in methylene chloride gives N-(2-aminoethyl)isoquinoline-5-sulfonamide (III), which is then condensed with S-methylisothiourea sulfate (IV) by means of NaOH at 80 C.
| 【1】 Asano, T.; Hidaka, H.; Vasodilatory action of HA-1004 [N-(2-guanidinoethyl)-5-isoquinolinesulfonamide], a novel calcium antagonist with no efect on cardiac function. J Pharmacol Exp Ther 1984, 231, 1, 141. |
| 【2】 Koch, H.; Castaner, J.; HA-1004. Drugs Fut 1985, 10, 10, 815. |
| 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) | 27362 | 5-isoquinolinesulfonyl chloride | 84468-15-5 | C9H6ClNO2S | 详情 | 详情 |
| (II) | 14754 | ethylenediamine;1,2-Diaminoethane;ethane-1,2-diamine；1,2-Ethanediamine | 107-15-3 | C2H8N2 | 详情 | 详情 |
| (III) | 27363 | N-(2-aminoethyl)-5-isoquinolinesulfonamide | C11H13N3O2S | 详情 | 详情 | |
| (IV) | 10272 | [[Amino(imino)methyl]sulfanyl]methane | 2986-19-8 | C2H6N2S | 详情 | 详情 |
Extended Information