Microwave‐assisted synthesis and chiral HPLC separation of 18F‐labeled MaxiPost™. An agent for post‐stroke neuroprotection

The syntheses of (S)‐3‐(5‐chloro‐2‐methoxyphenyl)‐1,3‐dihydro‐3‐[¹⁸F]‐fluoro‐6‐(trifluoromethyl)‐1H‐indol‐2‐one was accomplished by the microwave assisted carrier‐added ¹⁸F fluorination of (R,S)‐3‐(5‐chloro‐2‐methoxyphenyl)‐1,3‐dihydro‐3‐chloro‐6‐(trifluoromethyl)‐1H‐indol‐2‐one, followed by chiral HPLC separation to afford the desired ¹⁸F‐labeled enantiomer in radiochemical yields of 5–15% (EOS) and synthesis and purification times of 60–67 min. Biodistribution studies in rodents were consistent with previously reported studies using racemic ¹⁸F‐radiolabeled material. Copyright © 2003 John Wiley & Sons, Ltd.