This Primer Review is designed to give a succinct overview of the chemistry and pharmacology of psychedelics. It is hoped that it will provide a useful resource for science undergraduates, postgraduates and their instructors, and experienced scientists who require a comprehensive and up-to-date introduction to the field.

Preliminary evidence suggests that the active compound in ‘magic mushroom’, psilocybin may be beneficial in treating a range of mental health conditions. However, how psilocybin works on the brain to treat anxiety and depression isn’t well understood. This review brings together our current knowledge about psilocybin’s mechanism of action and suggests potential directions psilocybin therapy may take in the future.

In this short primer we will discuss the total synthesis of lysergic acid, an important precursor to lysergic acid diethylamide (LSD). Lysergic acid is also noted as a precursor for many drugs targeting the serotonin receptor family of GPCRs, including multiple known hallucinogens. We will discuss total syntheses containing B, C and D-ring cyclisations as the key step.

Homochiral R- and S-MDMA have been prepared by regioselective nucleophilic ring-opening of alanine-derived N-tosylaziridines.