Conditions for tandem, two step fluoroalkynylation of aryl halides with ?-alkynyl mesylates has been developed utilizing flow microreactor technology. With the production of radiotracers and radiopharmaceuticals relying on automated synthesis platforms for production, multi-step reactions performed in a continuous flow process are of great significance. Palladium catalyzed Sonogashira couplings of ?-alkynyl mesylates with aryl halides have been developed in a flow process under copper free conditions. Sensitive to the half life of fluorine-18 and to the homogeneity required for most flow processes, this two step continuous reaction was optimized for coupling and subsequent fluorination, which was executed in less than 30 minutes, without the need for ligand, copper, or amine.

Palladium catalyzed fluoroalkylations of aryl halides utilizing continuous flow microreactor technology

243rd National Meeting (2012)

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