The synthesis of 4-arylsulfanyl-substituted kainoid analogues from trans-4-hydroxy-L-proline

被引:13
作者
Baldwin, JE [1 ]
Pritchard, GJ [1 ]
Williamson, DS [1 ]
机构
[1] Univ Oxford, Dyson Perrins Lab, Oxford OX1 3QY, England
关键词
D O I
10.1016/S0960-894X(00)00352-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The potent neuroexcitatory activity of kainoid amino acids in the mammalian CNS places new analogues in high demand as tools ibr neuropharmacological research. A range of 4-arylsulfanyl-substituted kainoids has been synthesised in a parallel Fashion via mesylate displacement by a number of aromatic and heteroaromatic thiolates upon (2S,3S,4R)-1-benzoyl-3-tert-butoxycarboxylmethy-4-methanesulfonyloxy pyrrolidine-2-carboxylic acid methyl ester 8, which is obtainable in eight steps from trans-4-hydroxy-L-proline 5. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1927 / 1929
页数:3
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