专利号:US-6251689-B1 优先权日:1998-05-14 标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof 发明人:LABORDE EDGARDO; MATSUMOTO YUKIHARU 权利人:TELIK INC 摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
专利号:US-2023202980-A1 优先权日:2019-08-30 标题:N-(2-Aminophenyl)-Prop-2-Enamide Derivatives, and Uses Thereof in the Treatment of Cancer 发明人:RADHAKRISHNAN SRIDHAR; TENEN DANIEL G; LIU BEE HUI; VU LE KIM ANH; GO MEI LIN; CHAI LI; GAO CHONG; KAMAL AHMED; SUNKARI SATISH; AYINAMPUDI VENKATA SUBBARAO; SYED RIYAZ; LIU MIAO 权利人:NAT UNIV SINGAPORE; THE BRIGHAM AND WOMEN’S HOSPITAL INC; INDIAN INSTITUTE OF CHEMICAL TECH 摘要:Provided herein are N-(2-aminophenyl)-prop-2-enamide derivatives, such as those of Formula (I), methods for the synthesis thereof, and uses thereof in the treatment of cancer, such as SALL4-expressing cancer, in a cell or subject in need thereof.
专利号:US-10077242-B2 优先权日:2014-12-01 标题 :Convergent approach to the total synthesis of telmisartan via a suzuki cross-coupling reaction 发明人:GUPTON FRANK; MARTIN ALEX; SIAMAKI ALI; BELECKI KATHERINE 权利人:UNIV VIRGINIA COMMONWEALTH 摘要:Methods of synthesizing the angiotensin II receptor antagonist telmisartan in high yield and purity are provided. The methods involve the coupling of two structurally distinct benzimidazole units via a Suzuki cross-coupling reaction. Methods of regioselectively synthesizing one of the benzimidazole units are also provided.
专利号:US-11406964-B2 优先权日:2018-03-28 标题 :Heterogeneous catalysts for the synthesis of carbamates 发明人:WERSHOFEN STEFAN; VIDAL-FERRAN ANTON; RICO JOSÉ LUIS NÚÑEZ; PEREZ-RAMIREZ JAVIER; PUERTOLAS LACAMBRA BEGONA; AMRUTE AMOL P 权利人:COVESTRO INTELLECTUAL PROPERTY GMBH & CO KG 摘要:The present invention relates to a catalyst for preparing carbamates, in particular aromatic carbamates, comprising a binary oxide having the formula L1-xMxO2, wherein L is a metal selected from the lanthanoid series and M is a metal selected from the group consisting of Sc, Y, Ti, Zr, Hf, metals from the lanthanoid series and metals from the actinoid series, and wherein x ranges from 0.01 to 0.05. The present invention also relates to a method for producing said catalysts and a method of utilizing said catalysts in the production of carbamates, in particular aromatic carbamates.
专利号:US-3681297-A 优先权日:1970-11-10 标 题 :Synthesis of polybenzothiazolines and polybenzothiazoles by reacting a dialdehyde with an aromatic bis-mercaptoamine 发明人:ALELIO GAETANO FRANCIS D 权利人:GAETANO FRANCIS D ALELIO 摘要:THIS INVENTION DEALS WITH A NOVEL, RELATIVELY SIMPLE PROCESS OF PREPARING POLYBENZOTHIAZOLINES, ((-NH-CH(-)-S-)>AR<(-NH-CH(-Z(-))-S-))N BY REACTING DIALDEHYDES, Z-(CH=O)2, AND (HS)2-AR(-NH2)2 IN A SOLVENT IN AN INERT ATMOSPHERE AND THEREAFTER OXIDIZING THE POLYBENZOTHIAZOLINES TO POLYBENZOTHIAZOLES, ((-N=C(-)-S-)>AR<(-N=C(-Z(-))-S-))N WHEREIN AR REPRESENTS A TETRAVALENT AROMATIC MOIETY IN WHICH THE NITROGEN AND SULFUR ATOMS IN EACH PAIR ARE DISPOSED ORTHO TO EACH OTHER AND Z REPRESENTS A DIVALENT HYDROCARBON MOIETY AS THE RESIDUE OF THE DIALDEHYDE, Z(CHO)2. NEW TYPES, AS WELL AS THE KNOW TYPES OF POLYBENZOTHIAZOLES HAVE BEEN PREPARED BY THIS PROCESS.
专利号:US-3935314-A 优先权日:1971-11-24 标题 :Anti-hypertensive compositions of benzimidazole derivatives 发明人:WATTS ERIC ALFRED 权利人:BEECHAM GROUP LTD 摘要:Antihypertensive pharmaceutical compositions comprising a compound of the formula (II) ##SPC1## n or pharmaceutically acceptable salts or solvates thereof wherein R 1 is nitrile or amidino; R 2 is hydrogen or lower hydrocarbon; R 3 , R 4 , R 5 and R 6 which may be the same or different, are each selected from hydrogen, halogen, nitro, trifluoromethyl, lower alkyl, lower acyl, hydroxyl, lower etherified hydroxyl or lower acylated hydroxyl; together with a pharmaceutically acceptable carrier. The compounds of formula (II) are also useful as intermediates in the synthesis of the corresponding 2-aminoimidazoline compounds.
[参考文献]: Hizbullah Khan, Et Al. 1-Methyl-1H-Benzimidazole-2(3H)-Thione. Acta Crystallogr Sect E Struct Rep Online. 2008 May 24;64(Pt 6):O1141. [参考文献]: Tony Breton, Et Al. Modification Of Carbon Electrode With Aryl Groups Having An Aliphatic Amine By Electrochemical Reduction Of In Situ Generated Diazonium Cations. Langmuir. 2008 Aug 19;24(16):8711-8.
合成参考文献
摘要:Irudayanathan, F. M.; Lee, S., Science of Synthesis Knowledge Updates, (2019) 2, 20. 摘要:Irudayanathan, F. M.; Lee, S., Science of Synthesis Knowledge Updates, (2019) 2, 26. 摘要:Irudayanathan, F. M.; Lee, S., Science of Synthesis Knowledge Updates, (2019) 2, 19. 摘要:Irudayanathan, F. M.; Lee, S., Science of Synthesis Knowledge Updates, (2019) 2, 17. 摘要:Payne, P. R.; Gagné, M. R., Science of Synthesis: N-Heterocyclic Carbenes in Catalytic Organic Synthesis, (2016) 1, 377.