2-氯-6-甲氧基吡啶置于硫酸体系中,用80%的收率获得2-氯-6-甲氧基-3-硝基吡啶 参考文献:Novel Process For The Preparation Of 2-Halo-3-Nitro-6-Alkoxy-Pyridines 标题:Novel Process For The Preparation Of 2-Halo-3-Nitro-6-Alkoxy-Pyridines 摘要:一种简单的制备高纯度的1至6个烷氧基碳原子的2-卤代-3-硝基-6-烷氧基吡啶的新工艺,包括将2-卤代-6-烷氧基吡啶逐部分加入浓硫酸和浓硝酸混合物中,在0oc至40oc下得到不纯的2-卤代-3-硝基-6-烷氧基吡啶,然后用一种质子溶剂中的碱性反应化合物溶液处理后,回收所述吡啶,使其基本上处于纯净状态,这些化合物是镇痛药的重要中间体.
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:EP-2084147-B1 优先权日:2006-08-29 标 题:Heterocyclic fxr binding compounds 发明人:KREMOSER CLAUS; DEUSCHLE ULRICH; ABEL ULRICH; SCHULZ ANDREAS 权利人:PHENEX PHARMACEUTICALS AG 摘要:The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists or partial agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
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