Synthesis of α,β‐DI[3H]–2–fluoro–L–histidine
作者:
Kazuyuki Takahashi,
Kenneth L. Kirk,
Louis A. Cohen,
期刊:
Journal of Labelled Compounds and Radiopharmaceuticals
(WILEY Available online 1986)
卷期:
Volume 23,
issue 1
页码: 1-8
ISSN:0362-4803
年代: 1986
DOI:10.1002/jlcr.2580230102
出版商: John Wiley&Sons, Ltd.
关键词: 2‐Fluoro‐L‐histidine;fluoroimidazoles;azlactone synthesis;tritiation;metal‐halogen exchange;catalytic detritylation
数据来源: WILEY
摘要:
AbstractThe potent antimetabolite, 2‐fluoro‐L‐histidine, has been synthesized from 2‐fluoroimidazole with nonexchangeable3H labeling in the side chain. 2‐Fluoro‐4‐iodoimidazole was N‐tritylated, was subjected to metal‐halogen exchange with n‐butyllithium, and the carbanion formylated with DMF. The imidazole‐4‐aldehyde was condensed with hippuric acid, the azlactone was solvolyzed with methanol, and the trityl group was removed by selective reduction with PtS2. The resultinq 2‐fluoro‐α‐benzamidoacrylic ester was reduced with tritium gas and the blocking groups were removed successively with base and with acylase I to produce the L‐enantiomer
点击下载:
PDF
(314KB)
返 回