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:US-5869676-A 优先权日:1997-05-15 标题:Process for the synthesis of ribonucleotide reductase inhibitors 3-AP and 3-AMP 发明人:NIU CHUANSHENG; LI JUN; LI XIUYAN; DOYLE TERRENCE W; CHEN SHU-HUI 权利人:VION PHARMACEUTICALS INC 摘要:The present invention relates to improved, efficient chemical syntheses of 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) and 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP).
专利号:US-2012245199-A1 优先权日:2009-12-23 标题:[4 [4-(aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(1h-pyrrolo-pyridin-yl)-methanones and synthesis thereof 发明人:CHOI-SLEDESKI YONG MI; NIEDUZAK THADDEUS R; POLI GREGORY B; SHUM PATRICK WAI-KWOK; STOKLOSA GREGORY T; ZHAO ZHICHENG 权利人:CHOI-SLEDESKI YONG MI; NIEDUZAK THADDEUS R; POLI GREGORY B; SHUM PATRICK WAI-KWOK; STOKLOSA GREGORY T; ZHAO ZHICHENG; SANOFI SA 摘要:The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase.
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:US-5149814-A 优先权日:1987-09-30 标 题:Alkyl 2-benzylidene-4-(2-alkylimidazopyrid-1-yl) benzoylacetate esters as intermediate compounds 发明人:COOPER KELVIN; FRAY MICHAEL J; RICHARDSON KENNETH; STEELE JOHN 权利人:PFIZER 摘要:Intermediates useful in the synthesis of dihydropyridine platelet activating factor antagonists of the formula ##STR1## where R is phenyl or substituted phenyl; R 3 is lower alkyl; Y is 1,4-phenylene and X is 2-alkylimidazopyridyl.
专利号:CA-2657717-A1 优先权日:2006-07-15 标 题 :A regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles