In:
ChemMedChem, Wiley, Vol. 16, No. 21 ( 2021-11-05), p. 3271-3279
Abstract:
The efficient synthesis of L‐[5‐ 11 C]leucine and L‐α‐[5‐ 11 C]methylleucine has been investigated using a continuous two‐step sequence of rapid reactions consisting of Pd 0 ‐mediated 11 C‐methylation and microfluidic hydrogenation. The synthesis of L‐[5‐ 11 C]leucine and L‐α‐[5‐ 11 C]methylleucine was accomplished within 40 min with a decay‐corrected radiochemical yield of 15–38 % based on [ 11 C]CH 3 I, 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‐ 11 C]leucine or L‐α‐[5‐ 11 C]methyl leucine in A431 tumor‐bearing mice was performed. As a result, L‐α‐[5‐ 11 C]methylleucine was found to be a potentially useful probe for visualizing the tumor. Tissue distribution analysis showed that the accumulation value of L‐α‐[5‐ 11 C]methylleucine in tumor tissue was high [12±3% injected dose/g tissue (%ID/g)] .
Type of Medium:
Online Resource
ISSN:
1860-7179
,
1860-7187
DOI:
10.1002/cmdc.202100255
Language:
English
Publisher:
Wiley
Publication Date:
2021
detail.hit.zdb_id:
2209649-8
SSG:
15,3
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