公开(公告)号：US20240246937A1

公开(公告)日：2024-07-25

申请号：US18556196

申请日：2022-04-28

申请人： George Madalin GIAMBASU ,  Andrew M. HAIDLE ,  Brett A. HOPKINS ,  James P. JEWELL ,  Matthew A. LARSEN ,  Charles A. LESBURG ,  Ping LIU ,  Qinglin PU ,  Sulagna SANYAL ,  Phieng SILIPHAIVANH ,  Matthew TUDOR ,  Catherine M. WHITE ,  Xin YAN ,  Lianyun ZHAO ,  Xiao Mei ZHENG ,  William P. KAPLAN ,  Michaelyn Claire LUX ,  Derun LI ,  Rebecca JOHNSON ,  MERCK SHARP & DOHME LLC ,  MSD R&D (CHINA) CO., LTD.

发明人： George Madalin GIAMBASU ,  Andrew M. HAIDLE ,  Brett A. HOPKINS ,  James P. JEWELL ,  Matthew A. LARSEN ,  Charles A. LESBURG ,  Ping LIU ,  Qinglin PU ,  Sulagna SANYAL ,  Phieng SILIPHAIVANH ,  Matthew TUDOR ,  Catherine M. WHITE ,  Xin YAN ,  Lianyun ZHAO ,  Xiao Mei ZHENG ,  William P. KAPLAN ,  Michaelyn Claire LUX ,  Derun LI ,  Rebecca JOHNSON

IPC分类号： C07D403/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D487/04

CPC分类号： C07D403/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D487/04

摘要： The invention discloses a synthesizing method of benzimidazole derivant and intermediate, which is characterized by the following: proceeding arylation among aryl halide and primary amine; adopting L-pro as additive, cuprous iodide as catalyst; proceeding molecular arylation coupling reaction for aryl iodide or aryl bromide and primary amine; adopting iodo phenylamine compound and bromophenylamine compound as starting material; synthesizing the material through several-step transformation.