title: A General, One-Pot Method for the Synthesis of Sulfinic Acids from Methyl Sulfones.
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 and14C-labeling of several biologically active methyl sulfones were accessed via sulfinate intermediates.
authors.affiliation: Process Research & Development, Merck Research Laboratories, 126 East Lincoln Avenue, P.O. Box 2000, Rahway, New Jersey 07065, United States.
authors.forename: Donald R
authors.initials: DR
authors.lastname: Gauthier
authors.affiliation: Process Research & Development, Merck Research Laboratories, 126 East Lincoln Avenue, P.O. Box 2000, Rahway, New Jersey 07065, United States.
authors.forename: Naoki
authors.initials: N
authors.lastname: Yoshikawa