Azad Pharma Ag

Kristine Nerkararyan

Thomas Maier

Hartmut B Zinser

Mariam Gharibyan

Davit Hambardzumyan

Mikayel Movsisyan

Meri Grigoryan

Vahuni Karapetyan

Karine Barseghyan

Grigor Gevorgyan

Tamar Danielyan

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.

Process for the synthesis of buprenorphine

The present invention relates to a new path to synthesize crystalline Tafamidis polymorphs starting from a Tafamidis acetic acid adduct. In addition, this invention relates to a process to synthesize Tafamidis (2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid * (2R,3R,4R,5S)-6-(methyl-amino)-hexane-1,2,3,4,5-pentol), new Tafamidis crystalline polymorphs, a pharmaceutical compositions comprising the new crystalline polymorphs and to the therapeutic use of such new polymorphs.

Polymorphs and new path to synthesize Tafamidis

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Tavush, Armenia

Kristine Nerkararyan