CMI-977 is a potent 5-lipoxygenase inhibitor that intervenes
in the production of leukotrienes and is presently being
developed for the treatment of chronic asthma. It is a single
enantiomer with an all-trans (2S,5S) configuration. Of the four
isomers of CMI-977, the S,S isomer was found to have the best
biological activity and was selected for further development.
The enantiomerically pure product was synthesized on a 2-kg
scale from (S)-(+)-hydroxymethyl-γ-butyrolactone.
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