SYNTHESES OF 5-FLUORO-D/L-DOPA AND [F-18] 5-FLUORO-L-DOPA
SYNTHESES OF 5-FLUORO-D/L-DOPA AND [F-18] 5-FLUORO-L-DOPA
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DOI：
10.1016/0022-1139(93)03032-h
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发表时间：
1994-08-01
影响因子：
1.9
通讯作者：
WEINREICH, R
中科院分区：
文献类型：
--
作者：
ARGENTINI, M;WIESE, C;WEINREICH, R
以5-硝基香草醛为起始原料，经丙二酸酯合成、Balz-Schiemann反应和手性HPLC分离，合成了5-氟-D/L-多巴和相应的[F-18] 5-氟-L-多巴。经八步反应合成了无活性的5-氟-D/L-多巴，总收率为10%。为了可靠的合成，硝基用水合肼和活性炭上的钌还原。
This paper describes the synthesis of 5-fluoro-D/L-dopa and the corresponding [F-18]5-fluoro-L-dopa starting from 5-nitrovanillin via malonic ester synthesis, the Balz-Schiemann reaction and the separation of the racemic mixture [F-18]5-fluoro-D/L-dopa with a chiral HPLC system. The inactive 5-fluoro-D/L-dopa was obtained in an eight-step synthesis with an overall yield of 10%. For a reliable synthesis, the nitro group was reduced with hydrazine hydrate and ruthenium on charcoal.