专利号:US-8188282-B2 优先权日:2006-07-15 标 题:Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; HALLAND NIS; RKYEK OMAR; URMANN MATTHIAS 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; HALLAND NIS; RKYEK OMAR; URMANN MATTHIAS; SANOFI AVENTIS 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct palladium catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
专利号:EP-2173747-B1 优先权日:2007-06-26 标 题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; R KYEN OMAR; URMANN MATHIAS; HALLAND NIS 权利人:SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:AU-2007276514-A1 优先权日:2006-07-15 标题:A regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles
专利号:CA-2693142-A1 优先权日:2007-06-26 标题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles
专利号:CA-2657717-A1 优先权日:2006-07-15 标 题 :A regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles
专利号:AU-2008267443-A1 优先权日:2007-06-26 标 题 :A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles
参考标题: Proteasome Activity Enhancing Compounds Composés Renforçant L'Activité Des Protéasomes 摘要:The Present Invention Is Directed To Compounds Having The Formula (I), (II), (III), (Iv), And (V), Compositions Thereof, The Methods Of Synthesis Of The Compouds Of Interest, And To Methods For The Treatment Of A Condition Associated With A Dysfunction In Proteostasis, Such As Cancer, Inflammatory Conditions, Neurodegeneration, Metabolic Conditions, Comprising Administering An Effective Amount Of A Compound Of The Invention.
合成参考文献
参考文献:10.1007/s42452-025-06995-2 摘要:Snehalatha AV, Kumar NVA. Clinical trial of DprE1 inhibitors: from bench to bedside. Discov Appl Sci. 2025 May 09;7(5). doi: 10.1007/s42452-025-06995-2.