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【结 构 式】 
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【药物名称】L-Dopa ethyl ester, Etilevodopa, Levodopa ethyl ester, TV-1203 【化学名称】2(S)-Amino-3-(3,4-dihydroxyphenyl)propionic acid ethyl ester 【CA登记号】37178-37-3 【 分 子 式 】C11H15NO4 【 分 子 量 】225.2465 |
【开发单位】Teva (Proprietary), Hebrew University (Originator), Lundbeck (Licensee) 【药理作用】Antiparkinsonian Drugs, Chemical Delivery Systems, DRUG DELIVERY, Drug Delivery Systems, Extrapyramidal Disorders, Treatment of, NEUROLOGIC DRUGS, Dopamine Precursors |
合成路线1
Etilevodopa has been obtained by several different methods: (i) esterification of 3-hydroxy-L-tyrosine (I) (L-DOPA) with ethanol catalyzed by dry HCl gas; (ii) esterification of 3-hydroxy-L-tyrosine (I) (L-DOPA) by means of SOCl2 in hot ethanol; (iii) enzymatic hydroxylation of L-tyrosine ethyl ester (II) by means of mushroom tyrosinase in a phosphate buffer.
| 【1】 Sorbera, L.A.; Leeson, P.; Castaner, J.; Martin, L.; Etilevodopa. Drugs Fut 2001, 26, 3, 219. |
| 【2】 Ahmed, G.; Vulfson, E.N.; Facile synthesis of L-Dopa esters by the combined use of tyrosinase and alpha-chymotrypsin. Biotechnol Lett 1994, 16, 4, 367. |
| 【3】 Bahar, E.; Lidor, R.; Frenkel, A. (Teva Pharmaceutical Industries Ltd.; Teva Pharmaceuticals USA, Inc.); Process for manufacture of L-DOPA ethyl ester. US 6218566; WO 0027801 . |
| 【4】 Atlas, D.; Veinberg, A.; Melamed, E.; Milman, I. (Teva Pharmaceutical Industries Ltd.; Yissum Research Development Co.); Process for preparing ethyl ester of L-DOPA. EP 0610595; US 5354885 . |