Predominant Intramolecular Pummerer Reactions of Substituted Benzyl p-Tolyl Sulfoxides with Acetic Anhydride

Abstract
In the Pummerer reactions of 18O-labeled benzyl, and 3,5-dichlorobenzyl p-tolyl sulfoxides with a large excess of unlabeled acetic anhydride in the presence of DCC as acid scavenger, the resulted Pummerer reaction products, the α-acetoxy sulfides, were found to have retained substantial amounts of 18O-label of the original sulfoxides, i.e., nearly a half or more. Meanwhile, when optically active benzyl, 3-chlorobenzyl, and 3,5-dichlorobenzyl p-tolyl sulfoxides were allowed to react with excess acetic anhydride in the presence of DCC, the α-acetoxy sulfides, the Pummerer reaction products obtained, were found to have no optical activity. These observations suggest that the acetoxyl migration from sulfur atom to α-carbon is predominantly intramolecular, however, the α-(p-tolylthio) carbenium acetate ion-pair formed during the reaction prior to racemization is less intimate than those which are formed in the reactions of cyanomethyl and (α-carbonyl-substituted methyl) p-tolyl sulfoxides which give the corresponding highly optically active α-acetoxy sulfides.

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