公开(公告)号：EP4335853A2

公开(公告)日：2024-03-13

申请号：EP24152430.5

申请日：2021-01-27

申请人： AZAD Pharma AG

发明人： Zinser, Hartmut ,  Danielyan, Tamar ,  Grigoryan, Meri ,  Gharibyan, Mariam ,  Movsisyan, Mikayel ,  Nerkararyan, Kristine

IPC分类号： C07D498/12

摘要： 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.

公开(公告)号：EP4335853A3

公开(公告)日：2024-04-24

申请号：EP24152430.5

申请日：2021-01-27

申请人： AZAD Pharma AG

发明人： Zinser, Hartmut ,  Danielyan, Tamar ,  Grigoryan, Meri ,  Gharibyan, Mariam ,  Movsisyan, Mikayel ,  Nerkararyan, Kristine

IPC分类号： C07D498/12

CPC分类号： C07D498/12

摘要： 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.