The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Feb. 20, 2024
Filed:
Jan. 27, 2021
Azad Pharma Ag, Schaffhausen, CH;
Hartmut Zinser, Schaffhausen, CH;
Tamar Danielyan, Abovyan, AM;
Meri Grigoryan, Yerevan, AM;
Mariam Gharibyan, Yerevan, AM;
Mikayel Movsisyan, Yerevan, AM;
Kristine Nerkararyan, Yerevan, AM;
AZAD PHARMA AG, Schaffhausen, CH;
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.