Synthesis of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as potential prodrug of L-dopa
Synthesis of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as potential prodrug of L-dopa
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DOI：
10.1016/s0960-894x(00)00249-3
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发表时间：
2000-06-19
影响因子：
2.7
通讯作者：
Claudi, F
中科院分区：
文献类型：
--
作者：
Cingolani, GM;Di Stefano, A;Claudi, F
本文报道了左旋多巴前体药物L-（+）-3-（3-羟基-4-新戊酰氧基苄基）-2-5-二酮吗啉（9）的合成及其体外化学和酶促稳定性。前药9具有良好的亲脂性（log P = 2.153 +/-0.017），在水性缓冲溶液（pH 1.3和7.4）中稳定，并且在80%的大鼠和人血浆中其转化为L-多巴。(C)2000爱思唯尔科技有限公司版权所有。
The synthesis and in vitro chemical and enzymatic stability of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2-5-diketomorpholine (9) as L-Dopa prodrug are described. Prodrug 9 possesses a good lipophilicity (log P = 2.153 +/- 0.017), is stable in aqueous buffer solutions (pH 1.3 and 7.4), and in 80% rat and human plasma it is turned into L-Dopa. (C) 2000 Elsevier Science Ltd. All rights reserved.