Journal
ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 16, Issue 8, Pages 1393-1403Publisher
AMER CHEMICAL SOC
DOI: 10.1021/op300093j
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We describe the development of an efficient and scalable process for the preparation of fluorocyclobutane-containing H-3 antagonist, 1. The synthesis was accomplished by the chemoselective addition of a magnesium ate complex and an amine to a 1,4-ketoester in a one-pot sequence, followed by a diastereoselective carbonyl-directed fluorination. The chemoselective addition of the magnesium ate complex to the ketoester benefited from tight stoichiometric control, short addition times, and lower reaction temperatures, and thus was amenable to rapid mixing and excellent heat transfer in a flow reactor.
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