Organic & biomolecular chemistry

Synthesis of 18 F-labelled cyclooxygenase-2 (COX-2) inhibitors via Stille reaction with 4-[18 F] fluoroiodobenzene as radiotracers for positron emission tomography ( …

FR Wüst, A Höhne, P Metz

文献索引：Wuest, Frank R.; Hoehne, Aileen; Metz, Peter Organic and Biomolecular Chemistry, 2005 , vol. 3, # 3 p. 503 - 507

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被引用次数: 53

摘要

The Stille reaction with 4-[18F] fluoroiodobenzene as a novel approach for the synthesis of radiotracers for monitoring COX-2 expression by means of PET has been developed. Optimized reaction conditions were elaborated by screening of various catalyst systems and solvents. By using optimized reaction conditions 18F-labelled COX-2 inhibitors [18F]-5 and [18F]-13 could be obtained in radiochemical yields of up to 94% and 68%, respectively, ...