Conventional synthesis of glycosyl chlorides from thioglycosides relies on the two sequential oxidation and chlorination. A one-pot synthesis of glycosyl chlorides is warranted as an alternative method. Herein, we report the one-pot synthesis of glycosyl chlorides from thioglycoside precursors. The transformation was mediated at low temperature by bromodiethylsulfonium bromopentachloroantimonate (BDSB) as a mild oxidant and n-Bu4NCl as an additive. The armed thioglycosides afforded the corresponding α-glycosyl chlorides in moderate to good yields under the optimized conditions. Low conversions and yields were obtained when the less reactive disarmed thioglycosides were used. Unexpectedly, BDSB-mediated oxidation of thioglycosides without the addition of n-Bu4NCl also afforded the α-glycosyl chlorides in moderate yields. We suggest a mechanism involving the transfer of chloride ions from the non-nucleophilic bromopentachloroantimonate (SbCl5Br) anion to the oxocarbenium ion.
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