FLUOROACYLATION AGENTS BASED ON SMALL NCA [F-18] FLUOROCARBOXYLIC ACIDS
FLUOROACYLATION AGENTS BASED ON SMALL NCA [F-18] FLUOROCARBOXYLIC ACIDS
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DOI：
10.1016/0969-8043(94)90252-6
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发表时间：
1994-06-01
影响因子：
1.6
通讯作者：
STOCKLIN, G
中科院分区：
文献类型：
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作者：
GUHLKE, S;COENEN, HH;STOCKLIN, G
使用2-[F-18]氟代脂肪族酰基部分作为小辅基，比较了胺的氟酰化的三种方法。[F-18]氟乙酸和β-丙酸烷基酯是所有三种方法的常见中间体，并且以>90%的放射化学产率获得。它们可以直接用于伯胺的氟酰化。在第二种方法中，游离的[F-18]氟代脂肪酸与胺使用二环己基碳二亚胺（DCC）缩合。然而，副产物的形成将放射化学产率限制在约60%。或者制备咪唑或对硝基苯基酯和琥珀酰亚胺酯。在有机溶剂中，用这些高活性酯的氟酰化产率超过90%。二肽在水溶液中的氟酰化以70- 80%的产率进行。还制备了N-琥珀酰亚胺基4-[F-18]氟苯甲酸酯，放射化学产率（75%）比先前报道的高3倍。
Three methods for fluoroacylation of amines are compared using 2-[F-18]fluoroaliphatic acyl moieties as small prosthetic groups. [F-18]fluoroacetic and -propionic acid alkylesters are common intermediates for all three methods and obtained with >90% radiochemical yields. They can directly be used- for fluoroacylation of primary amines. In the second method the free [F-18]fluoroaliphatic acid is condensed with amines using dicyclohexyl carbodiimide (DCC). However, formation of byproducts limits the radiochemical yield to about 60%. Alternatively imidazolides or p-nitrophenyl and succinimidyl esters were prepared. Fluoroacylation yields with these highly activated esters exceed 90% in organic solvents. Fluoroacylation of dipeptides in aqueous solution proceeds with a yield of 70-80%. N-succinimidyl 4-[F-18]fluorobenzoate was also prepared with a 3-fold higher radiochemical yield (75%) than reported earlier.