An Improved, Practical, and Scalable Five-Step Synthesis of Psilocybin
Robert B. Kargbo, Alexander M. Sherwood, Poncho Meisenheimer, Gary Tarpley
Synthesis January 8, 2020 DOI: 10.1055/s-0039-1691565 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Chemical synthesis protocol Peer reviewed |
|---|---|
| Topics | Psilocybin |
| Keywords | Yield engineering Combinatorial chemistry Hallucinogen Pharmacology Alkaloids |
| Citations | 31 |
| Key points | An improved synthesis of psilocybin achieves 23% overall yield in five steps from an inexpensive acetoxyindole starting material without chromatography or aqueous workup. |
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.