专利号:US-8735586-B2 优先权日:2007-06-26 标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA 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 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: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:US-2010261909-A1 优先权日:2007-06-26 标题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles
专利号:WO-2009000413-A1 优先权日:2007-06-26 标题:A regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles
专利号:EP-2173721-B1 优先权日:2007-06-26 标 题:A regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles
专利号:KR-20100023907-A 优先权日:2007-06-26 标题:Regioselective Copper Catalytic Synthesis of Benzimidazole and Azabenzimidazole
[参考文献]: James R Vyvyan, Et Al. Suzuki-Miyaura Cross-Coupling Of 3-Pyridyl Triflates With 1-Alkenyl-2-Pinacol Boronates. Synthesis (Stuttg). 2010 Nov;2010(21):3637-3644.
合成参考文献
参考文献:10.1055/s-0040-1706870 摘要:Sabot C, Mabrouki A, Le Nahenec-Martel P, Kriaa A, Hedhli A, Renard P. Dearomatization of a 3-Hydroxypyridine Through an Unexpected Oxidative Deformylation Process: An Entry to Azacyclohexadienones. Synlett. 2020 Jul 13;31(15):1497–500. doi: 10.1055/s-0040-1706870.