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【结 构 式】

【药物名称】Enalapril maleate, MK-421, Ednit, Ditensor, Dabonal, Baripril, Crinoren, Xanef, Renitec, Enapren, Innovace, Innovace Melt(freeze-dried oral wafer), Lexxel(comb. with felodipine), Renivace, Vasotec

【化学名称】(S)-1-[N-[1-(Ethoxycarbonyl)-3-phenylpropyl]-L-alanyl]-L-proline maleate

【CA登记号】76095-16-4, 75847-73-3 (free base)

【 分 子 式 】C24H32N2O9

【 分 子 量 】492.53064

【开发单位】Merck & Co. (Originator), Merck Sharp & Dohme (Originator), Almirall Prodesfarma (Licensee), Banyu (Licensee), Uriach (Licensee), Vita (Licensee)

【药理作用】CARDIOVASCULAR DRUGS, Heart Failure Therapy, Hypertension, Treatment of, OCULAR MEDICATIONS, Ophthalmic Drugs, Angiotensin-I Converting Enzyme (ACE) Inhibitors

合成路线1

By reductocondensation of ethyl 2-oxo-4-phenylbutyrate (I) with alanylproline (II) by means of sodium cyanoborohydride or H2 over Raney-Ni or Pd/C in water.

1 Patchett, A.A.; et al.; A new class of angiotensin-converting anzyme inhibitors. Nature 1980, 288, 280-283.
2 Hopkins, S.J.; Serradell, M.N.; Blancafort, P.; Castaner, J.; Enalapril maleate. Drugs Fut 1982, 7, 8, 556.
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) 20896 Ethyl 2-oxo-4-phenylbutanoate; 2-Oxo-4-phenylbutyric acid ethyl ester 64920-29-2 C12H14O3 详情 详情
(II) 32151 (2S)-1-[(2S)-2-aminopropanoyl]-2-pyrrolidinecarboxylic acid 13485-59-1 C8H14N2O3 详情 详情
Extended Information