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Synthesis of a deuterium‐labelled standard of bufotenine (5‐HO‐DMT)

Yu Yun Wang, Chinpiao Chen

Journal of Labelled Compounds and Radiopharmaceuticals October 1, 2007 DOI: 10.1002/jlcr.1459 (opens in new tab)

Study at a glance

AI-extracted from the abstract
Characteristics Synthetic chemistry paper Peer reviewed
Topics DMT
Keywords Deuterium Stereochemistry Radiochemistry Nuclear physics
Citations 6
Key points Deuterium-labeled bufotenine was synthesized via the Batcho–Leimgruber strategy using lithium aluminum [2H4]-hydride to introduce four deuterium atoms.

Abstract

Abstract The Batcho–Leimgruber strategy was employed to synthesize 3‐(2‐dimethylamino‐[ 2 H 4 ]‐ethyl)‐1 H ‐indol‐5‐ol (bufotenine, 5‐HO‐DMT) ( 8 ) from commercial 3‐methyl‐4‐nitro‐phenol ( 1 ), benzyl bromide and N,N –dimethylformamide–dimethylacetal. Compound 4 was synthesized from compound 3 using the Batcho–Leimgruber strategy in the presence of Raney nickel and hydrazine hydrate. Compound 4 was treated with oxalyl chloride, dimethylamine and lithium aluminum [ 2 H 4 ]‐hydride to yield [2‐(5‐benzyloxy‐1 H ‐indol‐3‐yl)‐[ 2 H 4 ]‐ethyl]‐dimethyl‐amine ( 7 ). The benzyl ether in compound 7 was cleaved by hydrogenolysis to give bufotenine 8 . Copyright © 2007 John Wiley & Sons, Ltd.