Pyridine-3-Ylglyoxal置于聚合甲醛,氨体系中,用 水,二甲基亚砜 作为反应溶剂,化学反应生成 3-(1H-咪唑-4-基)吡啶 参考文献:Production Methods Of Imidazole Compound And Salt Thereof And Intermediates Therefor 标题:Production Methods Of Imidazole Compound And Salt Thereof And Intermediates Therefor 摘要:一种生产方法,包括将式(6)的卤素化合物或其盐在二甲基亚砜中转化为式(2)的甘醛化合物或其盐的步骤,以及将在前一步骤中获得的式(2)的甘醛化合物或其盐与氨和式(3)的醛化合物或其盐反应的步骤,可以方便地生产式(1)的咪唑化合物或其盐.该咪唑化合物是一种作为药物和农业化学品有用的化合物的合成中间体.该生产方法适用于工业规模生产.其中每个符号如规范中所定义.
专利号:US-9458111-B2 优先权日:2010-07-29 标题:Process for the synthesis of substituted urea compounds 发明人:LEARMONTH DAVID ALEXANDER; BROADBELT BRIAN; WAHNON JORGE BRUNO REIS 权利人:LEARMONTH DAVID ALEXANDER; BROADBELT BRIAN; WAHNON JORGE BRUNO REIS; BIAL—PORTELA & CA S A 摘要:A process for preparing a substitute urea of Formula (II) or Formula (I), or a pharmaceutically acceptable salt or ester thereof: n nthe process comprising the reaction of a carbamate of Formula (II′): Formula (I′):n n nwith a primary or secondary amine of the formula R1R2NH, wherein ring A, and R1, R2, R5, V, W, X, Y and Z are as defined herein.
专利号:US-11078163-B2 优先权日:2014-01-24 标 题 :Processes for the synthesis of substituted urea compounds 发明人:RUSSO DOMENICO; WAHNON JORGE BRUNO REIS; MATON WILLIAM; ESZENYI TIBOR 权利人:BIAL PORTELA & CA SA; BIAL PORTELA & Cª S A 摘要:The present invention concerns a process for preparing a compound having the Formula A; or a pharmaceutically acceptable salt or derivative thereof, or for preparing a substituted urea compound of Formula IIa, or a pharmaceutically acceptable salt or ester thereof, the process comprising the reaction of an imidazolyl intermediate of Formula IIa′ with a carbamoyl halide of the formula: R1R2NC(â• O)Hal, wherein Hal represents Cl, F, I or Br, wherein the intermediate of Formula IIa′ is prepared by oxidation of the derivative of R5 and R6, R6-C(â• O)CH2R5 to form a glyoxal intermediate R6-C(â• O)(Câ• O)R5, which is subjected to treatment with ammonium hydroxide and an aldehyde R8CHO to provide the intermediate of Formula IIa′ and wherein the compound substituents are as defined herein.
专利号:US-2015197503-A1 优先权日:2012-07-27 标题 :Process for the synthesis of substituted urea compounds 发明人:RUSSO DOMENICO; WAHNON JORGE BRUNO REIS; MATON WILLIAM; ESZENYI TIBOR 权利人:BIAL PORTELA & Cª S A 摘要:A process for preparing a substituted urea compound of Formula II or Formula I, or a pharmaceutically acceptable salt or ester thereof, Formula II, Formula I the process comprising the reaction of an intermediate of Formula II′ or Formula 1′, Formula II′, Formula I′ with a carbamoyl halide of the formula: R1R2NC(=0)Hal, in a solvent consisting essentially of pyridine, wherein Hal represents Cl, F, I or Br, and wherein ring A, and R1, R2, R5, V, W, X, Y and Z are as defined herein.
专利号:WO-2004046131-A1 优先权日:2002-11-20 标 题:Process for preparation of imidazoles and salts thereof and intermediates thereof 发明人:SHINTAKU TETSUYA; ITAYA NOBUSHIGE 权利人:SUMIKA FINE CHEMICALS CO LTD 摘要:A process which makes it possible to prepare easily imidazoles of the general formula (1) or salts thereof, which serve as intermediates in the synthesis of compounds useful as drugs or agricultural chemicals, and which is suitable for practice even on an industrial scale. The process comprises the step of converting a halide of the general formula (6) or a salt thereof in dimethyl sulfoxide into a glyoxal of the general formula (2) or a salt thereof and the step of reacting the glyoxal or salt thereof obtained in the above step with ammonia and an aldehyde of the general formula (3) or a salt thereof. (A) (In the formulae, each symbol is as defined in the description.)
专利号:US-2010286211-A1 优先权日:2004-10-08 标题:Oxazolidinone derivatives as antimicrobials 发明人:DAS BISWAJIT; AHMED SHAHADAL; YADAV AJAY SINGH; GHOSH SOMA; GUJRATI ARTI; SHARMA PANKAJ; RATTAN ASHOK 权利人:DAS BISWAJIT; AHMED SHAHADAL; YADAV AJAY SINGH; GHOSH SOMA; GUJRATI ARTI; SHARMA PANKAJ; RATTAN ASHOK 摘要:The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria, for example, multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, for example, Bacterioides spp. and Clostridia spp. species, and acid fast organisms, for example, Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
专利号:US-10995078-B2 优先权日:2013-03-13 标 题:Compounds and compositions for inhibition of FASN 发明人:BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J 权利人:FORMA THERAPEUTICS INC 摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below: