Synthesis and Characterization of 5-MeO-DMT Succinate for Clinical Use
Alexander M. Sherwood, Romain Claveau, Rafael Lancelotta, Kristi W. Kaylo, Kelsey Lenoch
ACS Omega December 2, 2020 DOI: 10.1021/acsomega.0c05099 via OpenAlex
Summary
AI-generated from the abstractA multigram-scale process was developed to produce 5-MeO-DMT, a psychedelic natural product from the toad Incilius alvarius, for clinical use. An optimized Fischer indole reaction yielded 5-MeO-DMT freebase, which was converted to the 1:1 succinate salt, producing 136 g of crystalline active pharmaceutical ingredient with 99.86% purity by HPLC and a net yield of 49%. The report details in-process monitoring, validated analytical methods, impurity formation and removal, and solid-state characterization essential for clinical development.
Study at a glance
| Characteristics | Process development report Peer reviewed |
|---|---|
| Keywords | Yield engineering High-performance liquid chromatography Salt chemistry Active ingredient Impurity |
| Citations | 38 |
| Key finding | A multigram-scale synthesis of 5-MeO-DMT succinate was achieved with 99.86% purity and 49% net yield, suitable for clinical use. |
Abstract
To support clinical use, a multigram-scale process has been developed to provide 5-MeO-DMT, a psychedelic natural product found in the parotid gland secretions of the toad, Incilius alvarius. Several synthetic routes were initially explored, and the selected process featured an optimized Fischer indole reaction to 5-MeO-DMT freebase in high-yield, from which the 1:1 succinate salt was produced to provide 136 g of crystalline active pharmaceutical ingredient (API) with 99.86% peak area by high-performance liquid chromatography (HPLC) and a net yield of 49%. The report provides in-process monitoring, validated analytical methods, impurity formation and removal, and solid-state characterization of the API essential for subsequent clinical development.