An efficient method for the synthesis of 3-mercapto-1-(1,3-thiazolin-2-YL)Azetidine useful for the pendant moiety of oral carbapenem, L-084
An efficient method for the synthesis of 3-mercapto-1-(1,3-thiazolin-2-yl)azetidine (1) is described. This thiol synthesis was achieved in 3 steps from readily available 3-methanesulfonyloxyazetidine via key intermediates, Bunte salts (3 and 5). The final step was enabled to proceed under mild conditions using the benzylthiol-mediated cleavage of the S-S bond in the Bunte salt (3).{A figure is presented}.
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