Process for the synthesis of buprenorphine
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United States of America Patent
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Feb 20, 2024
Grant Date -
Mar 9, 2023
app pub date -
Jan 27, 2021
filing date -
Jan 27, 2020
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Abstract
The present invention relates to a novel route of synthesis for the opioid receptor antagonist Buprenorphine or a pharmaceutically acceptable salt thereof, starting from thebaine, wherein the route comprises the reaction of thebaine with a dienophile; forming an alkylated reaction product by reaction with a Grignard-reagent; formation of an cyanamide; deprotection of the cyanamide- and the phenolic-oxygen-moiety, wherein the cleavage of one or both groups is performed in the presence of an alkali or alkaline earth sulfide; followed by derivatization with a cyclopropyl-halogen and hydrogenation to yield Buprenorphine.
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