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中山大学附属第一医院核医学科
纸质出版日期:2011-12-01
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[1]梁祥,王红亮,唐刚华,黄婷婷,吴克宁.(S-~(18)F-氟代甲基)-L-半胱氨酸的半自动化合成及其初步炎症PET显像[J].核技术,2011,34(12):937-942.
LIANG Xiang WANG Hongliang TANG Ganghua HUANG Tingting WU Kening. Semi-automated synthesis and preliminary inflammation PET study of(S-[18F]-fluoromethyl)-L-cysteine[J]. Nuclear techniques, 2011, 34(12): 937-942.
[1]梁祥,王红亮,唐刚华,黄婷婷,吴克宁.(S-~(18)F-氟代甲基)-L-半胱氨酸的半自动化合成及其初步炎症PET显像[J].核技术,2011,34(12):937-942. DOI:
LIANG Xiang WANG Hongliang TANG Ganghua HUANG Tingting WU Kening. Semi-automated synthesis and preliminary inflammation PET study of(S-[18F]-fluoromethyl)-L-cysteine[J]. Nuclear techniques, 2011, 34(12): 937-942. DOI:
改进现有合成模块
研究(S-
18
F-氟代甲基)-L-半胱氨酸(
F-MCYS)的自动化合成工艺
并对无菌炎症模型进行正电子发射断层(PET)显像。以CH
2
Br
为前体
经氟化反应制备甲基化试剂
F-CH
后者与溶解在二甲基亚砜(DMSO)中的L-半胱氨酸充分反应
用Sep-Pak C18小柱分离纯化
得到
F-MCYS注射液。
F-MCYS的未校正放化产率为(10.0±3.0)%(n=4
按
F计算)
放化纯度
>
95%
放化合成时间35 min。
F-MCYS可被炎症组织高度摄取
但不稳定
不适于PET显像研究。
Semi-automated synthesis of(S-[
l8
F]-fluoromethyl)-L-cysteine(
F-MCYS) was achieved with the modified commercial synthesizer and PET imaging of aseptic inflammatory mice was performed with
F-MCYS.
FCH
Br as
F-fluoromethylation agent was prepared by
F-fluorination of dibromomethane.
F-MCYS was obtained from the reaction of
Br with L-cysteine dissolved in dimethyl sulfoxide(DMSO) and purification on the solid-phase extraction cartridges.Without correction
the radiochemical yield of
F-MCYS was (10.0±3.0)%(n=4
based on
F )
the radiochemical purity of
F-MCYS was more than 95%
and the total synthesis time was about 35 min.It was found that
F-MCYS had high uptake in the inflammatory tissues
but
F-MCYS was unstable.Thus
F-MCYS is not a potential PET tracer for amino acid imaging and it is necessary for us to develop a novel stable
F-labelled cysteine.
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