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:US-2012172350-A1 优先权日:2009-09-11 标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
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:US-9096623-B1 优先权日:2014-05-08 标 题 :Method for preparing radiotracer precursor SnADAM 发明人:LEE CHING-YUN; CHANG YU; HSU CHENG-FANG; DENG YUEH-FENG 权利人:ATOMIC ENERGY COUNCIL—INST OF NUCLEAR ENERGY RES 摘要:A method for preparing a radiotracer precursor SnADAM is revealed. The method overcomes shortcomings of conventional synthesis methods including lower yield rate and time-consuming. Moreover, Pd/C catalyst and hydrogen gas are used to catalyze reduction reaction for avoiding the generation of a large amount of intermediate products with similar structures. Thus there is no need to perform isolation and purification processes. The yield rate of the intermediate products is also increased so that its impact on the low yield rate of the final product SnADAM is minimized. A part of the reaction is significantly accelerated by using tris(dibenzylideneacetone)-dipalladium(0) (Pd 2 (dba) 3 ) as a catalyst. Thus the production time of SnADAM is shortened.
专利号:AU-2008267444-A1 优先权日:2007-06-26 标 题 :A regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles