Finds effective chiral resolution of baclofen, suggesting a better method for preparing pure compounds.
An efficient large-scale preparation of enantiomerically pure ( R )- and ( S )-baclofen hydrochloride is described. The principal feature of this approach is the practical resolution of N-Boc-protected baclofen using 2-oxazolidinones as chiral auxiliaries, resulting in the formation of diastereomers, followed by crystallization separation, cleavage of Evans' oxazolidinone and deprotection of N-Boc group to yield baclofen enantiomers.
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Yang et al. (2026) studied this question.
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