ELECTROPHILIC SYNTHESIS OF 6-[F-18]FLUORO-L-DOPA - USE OF 4-O-PIVALOYL-L-DOPA AS A SUITABLE PRECURSOR FOR ROUTINE PRODUCTION

被引：13

作者：

ISHIWATA, K ^{[1
]}

ISHII, SI ^{[1
]}

SENDA, M ^{[1
]}

TSUCHIYA, Y ^{[1
]}

TOMIMOTO, K ^{[1
]}

机构：

[1] BANYU PHARMACEUT CO LTD,TSUKUBA RES INST,TSUKUBA 30033,JAPAN

来源：

APPLIED RADIATION AND ISOTOPES | 1993年 / 44卷 / 04期

关键词：

D O I：

10.1016/0969-8043(93)90144-Y

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

A method of 6-[F-18]fluoro-L-3,4-dihydroxyphenylalanine (6-[F-18]FDOPA) synthesis suitable for the routine production in human PET studies is described. Direct fluorination of L-3-(3-hydroxy-4-pivaloyloxyphenyl)alanine with acetyl [F-18]hypofluorite in acetic acid showed the preferable regioselectivity for 6-[F-18]FDOPA to its 2- and 5-fluoro isomers. The HCI-hydrolysis of the reaction mixture followed by HPLC separation using the buffered physiological saline as an eluting solution, gave a sterile and apyrogenic 6-[18]FDOPA injection for clinical studies: decay-corrected radiochemical yields of 15-21% based on acetyl [F-18]hypofluorite, radiochemical purity of > 97% and preparation time of 60 min.

引用

页码：755 / 759

页数：5

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