Process of synthesizing 2-bromo-LSD
View Patent ↗A process of synthesizing 2-bromo-LSD or a salt or hydrate thereof comprising the steps of reacting methylergometrine with a brominating agent to produce [(1S)-1-(Hydroxymethyl)propylamino][(6aR,9R)-5-bromo-7-methyl-4,7-diaza-4,6,6a,7,8,9-hexahydroacephenanthrylen-9-yl]formaldehyde as a first intermediate, and then hydrolyzing [(1S)-1-(Hydroxymethyl)propylamino][(6aR,9R)-5-bromo-7-methyl-4,7-diaza-4,6,6a,7,8,9-hexahydroacephenanthrylen-9-yl]formaldehyde to yield bromo-lysergic acid as a second intermediate, wherein bromo-lysergic acid is then amidated to yield 2-bromo-LSD or a salt or hydrate thereof.
1. A process of synthesizing 2-bromo-LSD or a salt or hydrate thereof comprising the steps of reacting methylergometrine with N-bromosuccinimide to produce [(1 S)-1-(Hydroxymethyl)propylamino][(6aR,9R)-5-bromo-7-methyl-4,7-diaza-4,6,6a,7,8,9-hexahydroacephenanthrylen-9-yl]formaldehyde, and then reacting [(1S)-1-(Hydroxymethyl)propylamino][(6aR,9R)-5-bromo-7-methyl-4,7-diaza-4,6,6a,7,8,9-hexahydroacephenanthrylen-9-yl]formaldehyde with a strong base to yield bromo-lysergic acid, wherein bromo-lysergic acid is then reacted with an acylating agent in the presence of an amine to yield 2-bromo-LSD or a salt or hydrate thereof.
2. The method of claim 1 , wherein the amine is diethylamine.
3. The method of claim 1 , wherein the amine is dimethylamine.
4. The method of claim 1 , wherein bromo-lysergic acid is reacted with POCl 3 and diethylamine.
5. The method of claim 4 , wherein a ratio of an amount of POCl 3 to an amount of bromo-lysergic acid ranges from about 1:1 to about 1:3.
6. The method of claim 1 , wherein the strong base is KOH.
7. A process of synthesizing 2-bromo-LSD or a salt or hydrate thereof comprising the step of reacting bromo-lysergic acid with POCl 3 and diethylamine, wherein a ratio of an amount of POCl 3 to an amount of bromo-lysergic acid ranges from about 1:1 to about 1:3.