An Improved, Practical, and Scalable Five-Step Synthesis of Psilocybin

2020/01/08 by Robert B. Kargbo, Alexander M. Sherwood, Poncho Meisenheimer +1 · 1 citation
Psychology · Chemistry · Pharmacology, Toxicology and Pharmaceutics · #Psychedelics and Drug Studies #Chemical synthesis and alkaloids #Alkaloids: synthesis and pharmacology

paper · pdf · doi:10.1055/s-0039-1691565

Abstract

Described herein is an improved synthesis of 3-[2-(dimethylamino)ethyl]-1H-indol-4-yl dihydrogen phosphate (psilocybin). The protocol outlines: synthesis of multigram quantities of psilocybin, identification of critical in-process parameters, and isolation of psilocybin without the use of chromatography, TLC, or aqueous workup. The synthesis furnishes psilocybin in five steps in 23% overall yield from an inexpensive acetoxyindole starting material. With specific focus on process control and impurity fate and removal, the improved procedure is amenable to providing high-quality psilocybin.

Citations

• Improvements to the Synthesis of Psilocybin and a Facile Method for Preparing the O-Acetyl Prodrug of Psilocin
• Pilot Study of Psilocybin Treatment for Anxiety in Patients With Advanced-Stage Cancer
• Psychiatry & the psychedelic drugs. Past, present & future

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• Psilocybin promotes neuroplasticity and induces rapid and sustained antidepressant-like effects in mice

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