کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10730489 | 1042558 | 2011 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Automated radiochemical synthesis of [18F]FBEM: A thiol reactive synthon for radiofluorination of peptides and proteins
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
فیزیک و نجوم
تشعشع
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چکیده انگلیسی
The automated radiochemical synthesis of N-[2-(4-[18F]fluorobenzamido)ethyl]maleimide ([18F]FBEM, IUPAC name: N-maleoylethyl-4-[18F]fluorobenzamide), a prosthetic group for radiolabeling the free sulfhydryl groups of peptides and proteins, is herein described. 4-[18F]fluorobenzoic acid was first prepared by nucleophilic displacement of a trimethylammonium moiety on a pentamethylbenzyl benzoate ester with [18F]fluoride. In the second step the ester was cleaved under acidic conditions. Finally, 4-[18F]fluorobenzoic acid was coupled to N-(2-aminoethyl)maleimide using diethylcyanophosphate and diisopropylethyl amine. Following high-performance liquid chromatography (HPLC) purification, [18F]FBEM was obtained in 17.3±7.1% yield (not decay corrected) in approximately 95 min. Isolation from the HPLC eluate and preparation for subsequent use, which was conducted manually, required an additional 10-15 min. The measured specific activity for three batches was 181.3, 251.6, and 351.5 GBq/ μmol at the end of bombardment (EOB).
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Applied Radiation and Isotopes - Volume 69, Issue 2, February 2011, Pages 410-414
Journal: Applied Radiation and Isotopes - Volume 69, Issue 2, February 2011, Pages 410-414
نویسندگان
Dale O. Kiesewetter, Orit Jacobson, Lixin Lang, Xiaoyuan Chen,