Synthesis and anticonvulsant activities of (R)-(O)-methylserine derivatives

被引：25

作者：

Andurkar, SV

Stables, JP

Kohn, H

机构：

[1] Univ Houston, Dept Chem, Houston, TX 77204 USA

[2] NINDS, Epilepsy Branch, NIH, Bethesda, MD 20892 USA

来源：

TETRAHEDRON-ASYMMETRY | 1998年 / 9卷 / 21期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1016/S0957-4166(98)00403-0

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Efficient procedures for the synthesis of (R)-N-benzyl-2-amino-3-methoxypropionamide ((R)-3), 2-acetamido-3-methoxypropionic acid (4), and O-methylserine (5) are described beginning from (R)-Cbz-serine ((R)-7). The reactions proceeded with little or no racemization and permitted the synthesis of the potent anticonvulsant (R)N-benzyl-2-acetamido-3-methoxypropionamide ((R)-2). The anticonvulsant activities of 2-4 were determined revealing the surprising activity of (R)-2. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：3841 / 3854

页数：14