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【结 构 式】 
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【药物名称】PNU-83757, U-83757, P-1075 【化学名称】1-Cyano-2-(1,1-dimethylpropyl)-3-(3-pyridyl)guanidine 【CA登记号】60559-98-0 【 分 子 式 】C12H17N5 【 分 子 量 】231.30279 |
【开发单位】Leo (Originator), Pfizer (Not Determined) 【药理作用】Antiarrhythmic Drugs, CARDIOVASCULAR DRUGS, Hypertension, Treatment of, RENAL-UROLOGIC DRUGS, Treatment of Erectile Dysfunction, Treatment of Male Sexual Dysfunction, K(ATP) Channel Activators |
合成路线1
Thiourea (III) was prepared by condensation of 3-pyridyl isothiocyanate (I) with 1,1-dimethylpropyl amine (II). Desulfuration of thiourea (III) by means of phosgene and diisopropyl ethylamine, or triphenylphosphine and CCl4 gave rise to the carbodiimide (IV). Finally, addition of cyanamide to carbodiimide (IV) furnished the target N-cyanoguanidine derivative
| 【1】 Manley, P.W.; Quast, U.; Structure-activity studies of potassium channel opening in pinacidil-type cyanoguanidines, nitroethenediamines, thioureas, and ureas. J Med Chem 1992, 35, 12, 2327. |
| 【2】 Petersen, H.J. (Leo Pharmaceutical Products Ltd. A/S); Antihypertensive pyridylguanidine compounds. DE 2557438; FR 2294703; GB 1489879; JP 51086474; US 4057636 . |