Title of article :
Synthesis of 4-(5-[18F]fluoromethyl-3-phenylisoxazol-4-yl)benzenesulfonamide, a new [18F]fluorinated analogue of valdecoxib, as a potential radiotracer for imaging cyclooxygenase-2 with positron emission tomography
Author/Authors :
Tatsushi Toyokuni، نويسنده , , J.S. Dileep Kumar، نويسنده , , Joseph C. Walsh، نويسنده , , Alan Shapiro، نويسنده , , John J. Talley، نويسنده , , Michael E. Phelps، نويسنده , , Harvey R. Herschman، نويسنده , , Jorge R. Barrio، نويسنده , , Nagichettiar Satyamurthy، نويسنده ,
Abstract :
Fluoroalkyl and fluoroaryl analogues of valdecoxib were found to possess potent inhibitory activities against cyclooxygenase-2 comparable to that of the parent valdecoxib. Among them, the fluoromethyl analogue was chosen for 18F-labeling. Thus, 4-(5-[18F]fluoromethyl-3-phenylisoxazol-4-yl)benzenesulfonamide ( 2000 Ci/mmol at end of synthesis) was synthesized by [18F]fluoride-ion displacement of the corresponding tosylate in 40% decay-corrected radiochemical yield within 120 min from end of bombardment.
