Journal
CHEMMEDCHEM
Volume 16, Issue 21, Pages 3271-3279Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.202100255
Keywords
amino acids; C-11-methylation; microfluidic hydrogenation; isotopic labeling; tumor imaging
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Funding
- Ministry of Education, Culture, Sport, Science and Technology (MEXT), (Japan)
- RIKEN
- JSPS KAKENHI Grant [JP19 K17184]
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Efficient synthesis of L-[5-C-11]leucine and L-alpha-[5-C-11]methylleucine was achieved using a two-step sequence, with promising potential of L-alpha-[5-C-11]methylleucine as a probe for visualizing tumors confirmed through tissue distribution analysis.
The efficient synthesis of L-[5-C-11]leucine and L-alpha-[5-C-11]methylleucine has been investigated using a continuous two-step sequence of rapid reactions consisting of Pd-0-mediated C-11-methylation and microfluidic hydrogenation. The synthesis of L-[5-C-11]leucine and L-alpha-[5-C-11]methylleucine was accomplished within 40 min with a decay-corrected radiochemical yield of 15-38 % based on [C-11]CH3I, radiochemical purity of 95-99 %, and chemical purity of 95-99 %. The Pd impurities in the injectable solution measured using inductively coupled plasma mass spectrometry met the international criteria for human use. Positron emission tomography scanning after an intravenous injection of L-[5-C-11]leucine or L-alpha-[5-C-11]methyl leucine in A431 tumor-bearing mice was performed. As a result, L-alpha-[5-C-11]methylleucine was found to be a potentially useful probe for visualizing the tumor. Tissue distribution analysis showed that the accumulation value of L-alpha-[5-C-11]methylleucine in tumor tissue was high [12 +/- 3% injected dose/g tissue (%ID/g)].
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