Efficient methods for the synthesis of 5-(4-[<SUP>18</SUP>F]fluorophenyl)-10,15,20-tris(3-methoxyphenyl) porphyrin as a potential imaging agent for tumor

초록

F-18-labeled porphyrins, the potential tracing and detecting agents for tumor have been synthesized and characterized by two convenient routes: one is a mixed aldehyde condensation, which involves acid-catalyzed condensation of pyrrole, m-anisaldehyde and 4-[F-18]fluorobenzaldehyde. The other is the acid-catalyzed condensation of tetrapyrrane with 4-[F-18]fluorobenzaldehyde. The synthetic methodologies including solvents, reaction concentrations and catalysts are optimized for radiolabeled porphyrins. The methods also provide the desired product in reasonable radiochemical yield (20-26%) compared with those of cold chemical synthesis (1-3%) and with high radiochemical purity (> 95%). The methods described here would be effective and convenient ways to produce radiolabeled porphyrin. Copyright (c) 2005 John Wiley & Sons, Ltd.

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