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A Successful Application of Phosphazene Base P2‐tBu to [11C]ABP688 Radiosynthesis in Fully Automated Synthesis Module
Bulletin of the Korean Chemical Society ( IF 1.7 ) Pub Date : 2020-08-16 , DOI: 10.1002/bkcs.12070
Jihye Lee 1
Affiliation  

[11C]ABP688 is the radioligand widely used for metabotropic glutamate subtype 5 (mGluR5) imaging in positron emission tomography (PET). The successful production of [11C]ABP688 in commercial automated synthesis module with hindered strong organic base was achieved. I compared 1,8‐bis(tetramethylguanidino)naphthalene (TMGN), tert‐butylimino‐tri(pyrrolidino)phosphorane (BTPP), P2‐tBu, P4‐tBu, and NaH as a base for C‐11 methylation of oxime and found P2‐tBu would be a suitable alternative for the conventional inorganic bases (NaH or NaOH). Considering the GMP application, P2‐tBu can provide compatibility with automated synthesizer and the resulting reliable synthesis. Three batches of the optimized condition for [11C]ABP688 synthesis were examined for quality assurance.

中文翻译:

磷腈基P2-tBu在全自动合成模块中成功应用于[11C] ABP688放射合成

[ 11 C] ABP688是放射性配体,广泛用于正电子发射断层扫描(PET)中的代谢型谷氨酸5型(mGluR5)成像。成功实现了商用自动合成模块中[ 11 C] ABP688的强有机碱受阻的生产。我比较了1,8-双(四甲基胍基)萘(TMGN),叔丁基亚氨基三(吡咯烷基)膦(BTPP),P2-tBu,P4-tBu和NaH作为肟C-11甲基化的基础P2-tBu将是常规无机碱(NaH或NaOH)的合适替代品。考虑到GMP应用程序,P2-tBu可提供与自动合成器的兼容性以及由此产生的可靠合成。针对[ 11检查了C] ABP688合成的质量保证。
更新日期:2020-08-16
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