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Chiral Switches of Tramadol Hydrochloride, a Potential Psychedelic Drug-Past and Future
Israel Agranat1, Ilaria D'Acquarica2
1Organic Chemistry, Institute of Chemistry, The Hebrew University of Jerusalem, Edmond J. Safra Campus, Jerusalem 9190401, Israel.
Abstract:
The chiral opioid analgesic tramadol was patented (1962) as a cis- and trans-racemates mixture. A first chiral switch led to the (±)-cis-(1RS,2RS) racemate, patented and approved as Tramal (1980), preferred over the (+)-cis-(1R,2R)-enantiomer. Consecutive chiral switches of (±)-cis-tramadol to (+)-cis-(1R,2R)-tramadol/salts were patented. This Viewpoint calls for developing (+)-cis-(1R,2R)-tramadol medicines and recognizing tramadol medicines as potential psychedelics to overcome the spreading tramadol crisis.
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