Synthesis and Characterization of 5-MeO-DMT Succinate for Clinical Use

ACS Omega  – December 02, 2020

Source: OpenAlex

Summary

A high-yield process has been developed to produce 5-MeO-DMT, a psychedelic compound derived from the parotid glands of the toad *Incilius alvarius*. Utilizing an optimized Fischer indole reaction, this method achieved a net yield of 49%, generating 136 grams of crystalline active pharmaceutical ingredient (API) with an impressive purity of 99.86% as confirmed by high-performance liquid chromatography (HPLC). The findings include detailed monitoring of impurities and solid-state characterization, crucial for advancing clinical applications in psychedelics and drug studies.

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.

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