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【结 构 式】 
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【药物名称】Lisinopril, ICI-209K, MK-521, Doneka, Prinzide, Zestril, Longes, Coric, Acerbon, Vivatec, Carace, Prinivil 【化学名称】(S)-1-[N2-(1-Carboxy-3-phenylpropyl)-L-lysyl]-L-proline 【CA登记号】76547-98-3 【 分 子 式 】C21H31N3O5 【 分 子 量 】405.49832 |
【开发单位】Merck & Co. (Originator), Bristol-Myers Squibb (Marketer), AstraZeneca (Licensee), Shionogi (Licensee), Vita (Licensee) 【药理作用】Acute Myocardial Infarction, Treatment of, ANALGESIC AND ANESTHETIC DRUGS, Antimigraine Drugs, CARDIOVASCULAR DRUGS, ENDOCRINE DRUGS, Heart Failure Therapy, Hypertension, Treatment of, Migraine, Prophylactic Treatment of, Treatment of Diabetic Complications, Treatment of Disorders of the Coronary Arteries and Atherosclerosis, Angiotensin-I Converting Enzyme (ACE) Inhibitors |
合成路线1
The reductocondensation of N(epsilon)-tert-butoxycarbonyl-lysyl proline (I) with 2-oxobutyric acid (II) by means of sodium cyanoborohydride in water gives the protected compound (III), which is finally treated with HCl in ethyl acetate.
| 【1】 Wyvratt, M.J.; Harris, E.E.; Patchett, A.A.; Tristram, E.W. (Merck & Co., Inc.); Carboxyalkyl dipeptide derivs., process for preparing them and pharmaceutical compsn. containing them. EP 0012401 . |
| 【2】 Blancafort, P.; Castaner, J.; Sneddon, J.M.; Serradell, M.N.; MK-521. Drugs Fut 1983, 8, 11, 925. |
| 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) | 31108 | (2S)-1-[(2S)-2-amino-6-[(tert-butoxycarbonyl)amino]hexanoyl]-2-pyrrolidinecarboxylic acid | C16H29N3O5 | 详情 | 详情 | |
| (II) | 23959 | 2-oxo-4-phenylbutyric acid | C10H10O3 | 详情 | 详情 | |
| (III) | 31109 | (2S)-1-((2S)-6-[(tert-butoxycarbonyl)amino]-2-[[(1S)-1-carboxy-3-phenylpropyl]amino]hexanoyl)-2-pyrrolidinecarboxylic acid | C26H39N3O7 | 详情 | 详情 |