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SYNTHESIS AND DETERMINATION FOR ENANTIOMERIC PURITY OF 6-FLUORO-L-DOPA

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Author:
No author available
Journal Title:
ACTA PHARMACEUTICA SINICA
Issue:
10
DOI:
10.3321/j.issn:0513-4870.2001.10.005
Key Word:
6-氟-L-多巴;手性催化剂;相转移烷基化;对映纯度;HPLC法;手性流动相

Abstract: 目的合成6-氟-L-多巴(6-FDOPA),并测定其对映纯度.方法以硝基藜芦醛(2)为原料,经亲核取代、还原碘化、手性相转移催化烷基化等多步反应得新化合物2-(2-氟-4,5-二甲氧苄基)-N-(二苯基甲叉)甘氨酸叔丁酯(8),8经水解反应制备终产物6-FDOPA,用手性流动相和反相C18柱的HPLC法测定其对映纯度.结果合成6-氟-L-多巴总反应时间少于90 min,总产率约为33%,对映纯度大于95%.结论可大量合成6-FDOPA,使自动合成6-[18F]-L-多巴成为可能.为6-[18F]-L-多巴的放射化学合成及其对映纯度的测定提供了可靠的技术.

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