497066-08-7Relevant academic research and scientific papers
Radiosynthesis of 1-(4-(2-[18F] fluoroethoxy)benzenesulfonyl)-3-butyl urea: A potential β-cell imaging agent
Schirrmacher, Ralf,Weber, Michael,Schmitz, Alexander,Shiue, Chyng-Yann,Alavi, Abass A.,Feilen, Peter,Schneider, Stefan,Kann, Peter,Roesch, Frank
, p. 763 - 774 (2002)
Tolbutamide (1) is a sulfonurea agent used to stimulate insulin secretion in type 2 diabetic patients. Its analogue 1-(4-(2-[18F]fluoroethoxy)benzenesulfonyl)-3-butyl urea (3) was synthesized in overall radiochemical yields of 45% as a potential β-cell imaging agent. Compound 3 was synthesized by 18F-fluoroalkylation of the corresponding hydroxy precursor (2) with 2-[18F]fluoroethyltosylate in DMF at 120°C for 10 min followed by purification with HPLC in a synthesis time of 50 min. Insulin secretion experiments of the authentic 19F-standard compound on rat islets showed that the compound has a similar stimulating effect on insulin secretion as that of tolbutamide (1). The partition coefficient of compound 3 between octanol/water was determined to be 1.3 × 0.3 (n = 5). Copyright
