Efficient synthesis of optically active α-substituted glutamate analogs possessing α-hydroxymethyl and α-alkoxymethyl groups
Efficient synthesis of optically active α-substituted glutamate analogs possessing α-hydroxymethyl and α-alkoxymethyl groups
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DOI：
10.1016/s0040-4039(02)02810-1
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发表时间：
2003-02-03
影响因子：
1.8
通讯作者：
Ohfune, Y
中科院分区：
文献类型：
--
作者：
Kawasaki, M;Namba, K;Ohfune, Y
使用Strecker合成的不对称版本在短步骤中实现了（2 R）-α-（羟甲基）谷氨酸盐（1）（mGluR 2和3的选择性激动剂）的高度对映选择性合成。这被转化为它的α-甲氧基甲基-和α-苄氧基甲基衍生物2和3，可能的配体作为工具，研究谷氨酸受体，通过保护的空间位阻的氨基，通过相转移催化剂。(C)2003爱思唯尔科技有限公司。保留所有权利。
Highly enantioselective synthesis of (2R)-alpha-(hydroxymethyl)glutamate (1), a selective agonist of mGluR2 and 3, was achieved in short steps using an asymmetric version of the Strecker synthesis. This was converted into its alpha-methoxymethyl- and alpha-benzyloxymethyl derivatives 2 and 3, possible ligands as tools to investigate glutamate receptors, via protection of the sterically hindered amino group by means of phase transfer catalyst. (C) 2003 Elsevier Science Ltd. All rights reserved.