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Microwave-assisted One-pot Synthesis of N-succinimidyl-4-[18F]fluorobenzoate [18F]SFB
Published on: June 28, 2011
A General, One-Pot Method for the Synthesis of Sulfinic Acids from Methyl Sulfones
Donald R Gauthier1, Naoki Yoshikawa1
1Process Research & Development, Merck Research Laboratories, 126 East Lincoln Avenue, P.O. Box 2000, Rahway, New Jersey 07065, United States.
Abstract:
A simple and efficient method for converting methyl sulfones to sulfinic acids is described. The process involves alkylation with a benzylic halide, followed by in situ elimination of the resulting styrene in the presence of excess base to yield a sulfinic acid in a single reaction process. The usefulness of the alkylation-elimination sequence is demonstrated by generating a variety of sulfinic acids from methyl sulfones. Late stage functionalization and 14C-labeling of several biologically active methyl sulfones were accessed via sulfinate intermediates.
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