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Synthesis and Characterization of 5-MeO-DMT Succinate for Clinical Use Options
 
The Traveler
#1 Posted : 12/23/2020 2:05:52 PM

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Abstract wrote:
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.


https://pubs.acs.org/doi/10.1021/acsomega.0c05099


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benzyme
#2 Posted : 12/23/2020 3:50:57 PM

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The authors likely didn't investigate Scheme 1 enough; preventing PS cyclization is done by keeping reaction temps low (-20 C to 5 C); kinetics at low temps favor imine alkylation over cyclization, 60-90% yield. Probably would've been more successful using NaBH4 too.

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famine
#3 Posted : 1/15/2021 10:35:10 AM

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benzyme wrote:
The authors likely didn't investigate Scheme 1 enough; preventing PS cyclization is done by keeping reaction temps low (-20 C to 5 C); kinetics at low temps favor imine alkylation over cyclization, 60-90% yield. Probably would've been more successful using NaBH4 too.


You are right about low temperature required to slow down the PS product but NaBH4 isn't a good choice for any reductive amination. It reduces aldehydes and ketones Thumbs down NaBH3CN is great because it's strong enough to reduce the imine but not the aldehyde. It also requires less cooling. The NaBH4 route is good, if you're careful enough you can get 80% yield easily but it's just god damm tedious with all that cooling. You should try run this route but with STAB and anhydrous. Very easy to make from NaBH4 and no cooling is required. You just leave it to stir and get 90%+ Cool
 
 
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