- α-Bromoacrylic Acids as C1 Insertion Units for Palladium-Catalyzed Decarboxylative Synthesis of Diverse Dibenzofulvenes
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Herein α-bromoacrylic acids have been employed as C1 insertion units to achieve the palladium-catalyzed [4 + 1] annulation of 2-iodobiphenyls, which provides an efficient platform for the construction of diverse dibenzofulvenes. This protocol enables the formation of double C(aryl)-C(vinyl) bonds via a C(vinyl)-Br bond cleavage and decarboxylation. It is particularly noteworthy that the method features a broad substrate scope, and various interesting frameworks, such as bridged ring, fused (hetero)aromatic ring, and divinylbenzene, can be successfully incorporated into the products.
- Zhang, Minghao,Deng, Wenbo,Sun, Mingjie,Zhou, Liwei,Deng, Guobo,Liang, Yun,Yang, Yuan
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supporting information
p. 5744 - 5749
(2021/08/18)
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- Electrochemical Palladium-Catalyzed Intramolecular C—H Amination of 2-Amidobiaryls for Synthesis of Carbazoles
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The synthesis of carbazoles based on the electrochemical Pd-catalyzed intramolecular C—H amination of 2-amidobiaryls through oxidative cross coupling has been achieved under mild reaction conditions. The reaction can be carried out in undivided cell without the addition of external chemical oxidant. Besides good functional group compatibility, the desired carbazoles can be scaled up and modified easily. Compared with previous methods, this protocol affords a simple and sustainable avenue for the construction of carbazoles.
- Gao, Xinlong,Lei, Aiwen,Wang, Pan,Wang, Qingqing,Zhang, Heng,Zhang, Xiaojing
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supporting information
p. 143 - 148
(2020/12/18)
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- Self-Assembled Multilayer Iron(0) Nanoparticle Catalyst for Ligand-Free Carbon-Carbon/Carbon-Nitrogen Bond-Forming Reactions
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Self-assembled multilayer iron(0) nanoparticles (NPs, 6-10 nm), namely, sulfur-modified Au-supported Fe(0) [SAFe(0)], were developed for ligand-free one-pot carbon-carbon/carbon-nitrogen bond-forming reactions. SAFe(0) was successfully prepared using a well-established metal-nanoparticle catalyst preparative protocol by simultaneous in situ metal NP and nanospace organization (PSSO) with 1,4-bis(trimethylsilyl)-1,4-dihydropyrazine (Si-DHP) as a strong reducing agent. SAFe(0) was easy to handle in air and could be recycled with a low iron-leaching rate in reaction cycles.
- Akiyama, Toshiki,Arisawa, Mitsuhiro,Haneoka, Hitoshi,Harada, Kazuo,Hasegawa, Jun-Ya,Honma, Tetsuo,Mashima, Kazushi,Sato, Yoshihiro,Shimoda, Shuhei,Shio, Yasunori,Suzuki, Takeyuki,Tamenori, Yusuke,Tsurugi, Hayato,Tsuruta, Kazuki,Wada, Yuki,Yamada, Makito
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supporting information
p. 7244 - 7249
(2020/10/12)
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- Cascade One-Pot Synthesis of Orange-Red-Fluorescent Polycyclic Cinnolino[2,3-f]phenanthridin-9-ium Salts by Palladium(II)-Catalyzed C?H Bond Activation of 2-Azobiaryl Compounds and Alkenes
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Quaternary ammonium salts were synthesized in moderate to good yields through double oxidative C?H bond activation on azobenzenes. The mechanism of the highly regioselective reaction of 2-azobiaryls with alkenes to give orange-red-fluorescent cinnolino[2,
- Jayakumar, Jayachandran,Vedarethinam, Guganchandar,Hsiao, Huan-Chang,Sun, Shang-You,Chuang, Shih-Ching
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supporting information
p. 689 - 694
(2019/11/22)
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- Cobalt(II)-Catalyzed [5+2] C?H Annulation of o-Arylanilines with Alkynes: An Expedient Route to Dibenzo-[b,d]azepines
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The first example of CoCl2-catalyzed formal [5+2] oxidative annulation of o-arylanilines with alkynes was developed, giving access to various important imine-containing dibenzo-[b,d]azepine scaffolds through sequential C?C/C?N bond formation. The reaction employs catalytic amount of manganese and oxygen as cooxidants, and features a broad substrate scope. Preliminary mechanistic studies suggested that C?H activation is involved in the rate-determining step. Moreover, both internal and terminal alkynes are well tolerated in this transformation. Besides, a regioselective migratory insertion was observed when using terminal alkynes as substrates. (Figure presented.).
- Ling, Fei,Xie, Zhen,Chen, Jiachen,Ai, Chongren,Shen, Haiwei,Wang, Ze,Yi, Xiao,Zhong, Weihui
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supporting information
p. 3094 - 3101
(2019/05/21)
-
- FLUOROPHENYL SUBSTITUTED MUSCARINIC RECEPTOR LIGANDS WITH SELECTIVITY FOR M3 OVER M2
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The present invention relates to fluorophenyl substituted muscarinic receptor ligands with selectivity for M3 over M2 and to the use of these compounds in the treatment of various diseases such as asthma, chronic obstructive pulmonary disease (COPD), bronchopulmonary dysplasia (BPD) and urinary incontinence.
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Page/Page column 30; 44; 47; 48
(2019/06/23)
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- Effective bimetallic composite catalysts for the synthesis of arylated furans and thiophenes in aqueous media
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[Figure not available: see fulltext.] N-(4,6-Dimethylpyrimidin-2-yl)-5-phenylisoxazole-3-carboxamide was used as a ligand for obtaining bimetallic boron-containing heterogeneous catalysts Pd–Ni(Co)–B–L (Ni(Co):Pd = 9:1). The obtained composites were highl
- Bumagin, Nikolay A.,Petkevich, Sergey K.,Kletskov, Alexey V.,Alekseyev, Roman S.,Potkin, Vladimir I.
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- B2N2-Embedded Polycyclic Aromatic Hydrocarbons with Furan and Thiophene Derivatives Functionalized in Crossed Directions
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A series of polycyclic aromatic hydrocarbons (PAHs), consisting of two pairs of BN units, have been designed and their synthesis has been achieved by electrophilic C?H borylation. Two conjugation extension directions can be found in these B2Ns
- Chen, Yijing,Chen, Weinan,Qiao, Yanjun,Zhou, Gang
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p. 9326 - 9338
(2019/07/04)
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- Rhodium(I)-Catalyzed Aryl C-H Carboxylation of 2-Arylanilines with CO2
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An unprecedented Rh(I)-catalyzed, amino-group-assisted C-H carboxylation of 2-arylanilines with CO2 under redox-neutral conditions has been developed. This reaction was promoted by a phosphine ligand with t-BuOK as the base and did not require the use of additional strong organometallic reagent. It enabled an efficient direct conversion of a broad range of 2-(hetero)arylanilines including electron-deficient heteroarenes to various phenanthridinones. Possible intermediates of the reaction were also evaluated in the preliminary mechanistic studies.
- Gao, Yuzhen,Cai, Zhihua,Li, Shangda,Li, Gang
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supporting information
p. 3663 - 3669
(2019/05/17)
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- Metal- and additive-free cascade trifluoroethylation/cyclization of organic isoselenocyanates by phenyl(2,2,2-trifluoroethyl)iodonium triflate
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A novel and convenient cascade trifluoroethylation/cyclization of organic isoselenocyanates by phenyl(2,2,2-trifluoroethyl)iodonium triflate is reported. A series of 2-isoselenocyanobiaryls and aryl alkyl isoselenocyanates reacted with phenyl(2,2,2-trifluoroethyl)iodonium triflate in CH2Cl2 at 40 °C under metal- and additive-free conditions for 3 h to provide the corresponding trifluoroethylselenolated phenanthridines and 3,4-dihydroisoquinoline derivatives in good to excellent yields. The reaction represents the first general approach to access trifluoroethylselenolated phenanthridines and 3,4-dihydroisoquinolines from organic isoselenocyanates.
- Zhao, Cheng-Long,Shi, Jin,Lu, Xiuqiang,Wu, Xun,Zhang, Cheng-Pan
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supporting information
(2019/09/03)
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- Metal-Oxidant-Free Cobalt-Catalyzed C(sp2)-H Carbonylation of ortho-Arylanilines: An Approach toward Free (NH)-Phenanthridinones
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A traceless directing group assisted Co-catalyzed C(sp2)-H carbonylation of ortho-arylanilines for the synthesis of free (NH)-phenanthridinones in metal-based-oxidant-free fashion was accomplished. This protocol employs diisopropyl azodicarboxylate as the CO source and oxygen as the sole oxidant, and provides good yields with various functional tolerance. The methodology has been applied for the total synthesis of PARP inhibitor PJ-34. Furthermore, the kinetic isotopic effect experiments reveal the C-H bond cleavage probably occurred in the rate-determining step.
- Ling, Fei,Zhang, Chaowei,Ai, Chongren,Lv, Yaping,Zhong, Weihui
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p. 5698 - 5706
(2018/05/23)
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- Palladium(II)-catalyzed mono-and bis-alkenylation of N-acetyl-2-aminobiaryls through regioselective C-H bond activation
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We developed palladium-catalyzed oxidative coupling of olefins with N-acyl 2-aminobiaryls through a sequence of ortho C-H bond activation/alkene insertion/reductive elimination. Furthermore, we controlled the selectivity of mono-and bis-alkenylation products with the solvent effect. The developed protocol was promising for a broad substrate scope ranging from activated olefins with a wide variety of functional groups to unactivated olefins.
- Annamalai, Pratheepkumar,Hsu, Kou-Chi,Raju, Selvam,Hsiao, Huan-Chang,Chou, Chih-Wei,Lin, Gu-Ying,Hsieh, Cheng-Ming,Chen, Pei-Ling,Liu, Yi-Hung,Chuang, Shih-Ching
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p. 3840 - 3856
(2018/04/14)
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- Photochemical intramolecular amination for the synthesis of heterocycles
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Polycyclic heterocycles can be formed in good to excellent yields via photochemical conversion of the corresponding substituted aryl azides under irradiation with purple LEDs in a continuous flow reactor. The experimental set-up is tolerant to UV-sensitive functional groups while affording diverse carbazoles, as well as an indole and pyrrole framework, in short reaction times. The photochemical method is presumed to progress through a mechanism differing from the other methods of azide activation involving transition metal catalysis.
- Parisien-Collette, Shawn,Cruché, Corentin,Abel-Snape, Xavier,Collins, Shawn K.
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supporting information
p. 4798 - 4803
(2017/10/23)
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- 3,5-[5-Arylisoxazol-3-yl(4,5-dichloroisothiazol-3-yl)]-substituted 1,2,4- and 1,3,4-oxadiazoles: synthesis, palladium complexes, and catalysis of Suzuki reactions in aqueous media
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[Figure not available: see fulltext.] A reaction sequence involving transformations of 5-(4-methylphenyl)isoxazole and 4,5-dichloroisothiazole derivatives containing an amidoxime group at position 3 allowed to synthesize the respective 3,5-isoxazolyl(isothiazolyl)-substituted 1,2,4-oxadiazoles. Selective recyclization of 4,5-dichloro-3-(1Н-tetrazol-5-yl)isothiazole and 5-(4-methylphenyl)-3-(1Н-tetrazol-5-yl)isoxazole gave 2,5-isoxazolyl-(isothiazolyl)-substituted 1,3,4-oxadiazoles. The obtained compounds combining three azole heterocycles in one molecule formed palladium complexes that showed high catalytic activity in Suzuki reactions in aqueous and aqueous alcohol media. The bimetallic reusable Pd/Fe catalyst obtained from palladium polyazole complex retained high catalytic activity after five uses.
- Bumagin, Nikolay A.,Petkevich, Sergey K.,Kletskov, Alexey V.,Potkin, Vladimir I.
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p. 1340 - 1349
(2018/02/06)
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- Synthesis and Properties of New N-Heteroheptacenes for Solution-Based Organic Field Effect Transistors
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A series of N-heteroheptacenes was synthesized from ortho-thiophene-substituted aryl azides using a Rh2II-catalyzed C?H bond amination reaction to construct the thienoindole moieties. This reaction tolerated the presence of electron-
- Zhou, Fei,Liu, Sheng,Santarsiero, Bernard D.,Wink, Donald J.,Boudinet, Damien,Facchetti, Antonio,Driver, Tom
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supporting information
p. 12542 - 12549
(2017/09/18)
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- Pd/Cu-Catalyzed aerobic oxidative aromatic C-H bond activation/N-dealkylative carbonylation towards the synthesis of phenanthridinones
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It is important to achieve diverse functionalization of tertiary anilines due to their importance in biological molecules, pharmaceutical, functional materials, and ligands. A straightforward Pd/Cu-catalyzed oxidative C-H bond activation/N-dealkylative carbonylation of tertiary [1,1′-biphenyl]-2-anilines towards the synthesis of various biologically important phenanthridin-6(5H)-ones has been developed. A wide range of functional groups are well tolerated in this transformation. Moreover, O2 is utilized as the terminal oxidant to promote the oxidative carbonylation process.
- Shi, Renyi,Niu, Huiying,Lu, Lijun,Lei, Aiwen
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p. 1908 - 1911
(2017/02/10)
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- Palladium-Catalyzed C-H Bond Activation by Using Iminoquinone as a Directing Group and an Internal Oxidant or a Co-oxidant: Production of Dihydrophenanthridines, Phenanthridines, and Carbazoles
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A palladium-catalyzed C-H bond activation reaction, via a redox-neutral pathway, for the preparation of dihydrophenanthridine, phenanthridine, and carbazole derivatives from biaryl 2-iminoquinones is developed. The preinstalled iminoquinone was designed to act as a directing group for ortho C-H activation and an internal oxidant or a co-oxidant. This catalysis proceeded through the following sequence: C-H bond activation, coordination and insertion of activated olefins, β-hydride elimination, H-shift, insertion, and protonation or β-hydride elimination. In addition, carbazoles can be prepared efficiently by using this method without the addition of external oxidants.
- Raju, Selvam,Annamalai, Pratheepkumar,Chen, Pei-Ling,Liu, Yi-Hung,Chuang, Shih-Ching
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supporting information
p. 4134 - 4137
(2017/08/15)
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- High-turnover aminopyridine-based Pd-catalysts for Suzuki-Miyaura reaction in aqueous media
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A high-turnover catalytic system based on commercially available aminopyridines (L) and PdCl2 has been developed for Suzuki-Miyaura reaction in aqueous media. Reactions of arylboronic acids with a wide range of aryl iodides, bromides and chlorides proceeded in the presence of these catalysts for a short time in aqueous media to afford the cross-coupling products in high yields. Furthermore, this protocol allows tolerating a wide range of functional groups.
- Bumagin, Nikolay A.
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- Functionally substituted isoxazoles and isothiazoles: Synthesis, palladium(II) complexes and their catalytic activity
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Functionally substituted 5-(p-tolyl)isoxazoles and 4,5-dichloroisothiazoles, whose molecules contain azomethine, amino, carboxyl, and ester moieties in various combinations in the aromatic ring in the position 3 of heterocycle, were synthesized. Synthesis of complexes of Pd(II) with carboxyl derivative of 1,2-azoles was performed. They show high catalytic activity in the Suzuki reaction in aqueous media.
- Bumagin,Zelenkovskii,Kletskov,Petkevich,Dikusar,Potkin
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- Visible-light-photocatalyzed metal-free C-H heteroarylation of heteroarenes at room temperature: A sustainable synthesis of biheteroaryls
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An efficient C-H heteroarylation of heteroarenes is achieved through visible-light photoredox-catalyzed diazotization of heteroarylamines in situ by tBuONO at room temperature. A library of functionalized biheteroaryls is obtained by using this protocol.
- Maity, Pintu,Kundu, Debasish,Ranu, Brindaban C.
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p. 1727 - 1734
(2015/05/27)
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- Synthesis of 6-(arylthio)phenanthridines by copper-catalyzed tandem reactions of 2-biaryl isothiocyanates with diaryliodonium salts
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A novel copper-catalyzed tandem C-S/C-C bond-forming reaction of 2-biaryl isothiocyanates with diaryliodonium salts was developed. This is the first general approach to synthesize phenanthridines from 2-biaryl isothiocyanates. This methodology has been successfully applied to the synthesis of trisphaeridine.
- Guo, Weisi,Li, Shoulei,Tang, Lin,Li, Ming,Wen, Lirong,Chen, Chao
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supporting information
p. 1232 - 1235
(2015/03/14)
-
- Synthesis of 4-alkylidene-substituted 1,2,3,4-tetrahydroisoquinolines via palladium-catalyzed carbopalladation/C-H activation of 2-bromobenzyl-N-propargylamines
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Abstract Tetrasubstituted alkene-based 1,2,3,4-tetrahydroisoquinolines are synthesized via the formation of a cyclic carbopalladation complex followed by C-H bond activation of the sp2 carbon in arenes. This domino reaction proceeds with good selectivity and provides good yields of the products. The requisite starting materials are synthesized by copper(I) iodide catalyzed A3-coupling reactions.
- Naveen, Kanagaraj,Nandakumar, Avanashiappan,Perumal, Paramasivan Thirumalai
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supporting information
p. 1633 - 1642
(2015/03/31)
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- An effective activation of palladium phosphine complexes in aqueous phase reactions of hetero-aromatic boronic acids with aryl halides
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We have developed a simple and effective method for the activation of palladium phosphine complexes in the Suzuki reaction (TON up to 9800, TOF up to 58800 h-1) by selecting an aqueous reaction medium instead of organic solvents. This method wa
- Bumagin,Veselov,Belov
-
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- 5-(Naphth-1-yl)- and 5-[(1,1'-biphenyl)-4-yl]isoxazole-3-carbaldehyde oximes: Synthesis, complexes with palladium, and application in catalysis
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1-(Naphth-1-yl)- and 1-[(1,1'-biphenyl)-4-yl-3,4,4-trichloro-3-buten-1-ones were synthesized by acylation of naphthalene and biphenyl with 3,4,4-trichloro-3-butenoyl chloride. Further reaction with hydroxylamine led to 5-(naphth-1-yl)- and 5-[(1,1'-biphen
- Potkin,Bumagin,Zelenkovskii,Petkevich,Livantsov,Golantsov
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p. 1782 - 1792
(2015/01/08)
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- Synthesis of carbazoles by copper-catalyzed intramolecular C-H/N-H coupling
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A Cu-catalyzed intramolecular C-H amination for the synthesis of carbazoles has been developed. The key to success is the installation of the picolinamide-based directing group, which is spontaneously removed after the coupling event. The Cu catalysis proceeded smoothly under Pd- and I(III)-free conditions, and its mild oxidation aptitude enables the rapid and concise construction of heteroatom-incorporated carbazole core π-systems.
- Takamatsu, Kazutaka,Hirano, Koji,Satoh, Tetsuya,Miura, Masahiro
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supporting information
p. 2892 - 2895
(2014/06/23)
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- Pd(II)-catalyzed C(sp2)-H carbonylation of biaryl-2-amine: Synthesis of phenanthridinones
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A Pd(OAc)2-catalyzed C(sp2)-H carbonylation protocol of arenes under carbon monoxide atmosphere has been developed. The scope of the carbonylation reaction is broad and tolerates a variety of useful functional groups. This reaction provides a novel and efficient method for the synthesis of biologically and pharmaceutically significant phenanthridinones.
- Liang, Zunjun,Zhang, Jitan,Liu, Zhanxiang,Wang, Kai,Zhang, Yuhong
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p. 6519 - 6526
(2013/07/26)
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- PhI(OAc)2-mediated synthesis of 6-(trifluoromethyl) phenanthridines by oxidative cyclization of 2-isocyanobiphenyls with CF 3SiMe3 under metal-free conditions
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A mild and efficient method for the synthesis of 6-(trifluoromethyl) phenanthridines through oxidative cyclization of 2-isocyanobiphenyls with CF3SiMe3 under metal-free conditions was developed. The reaction allows the direct formation of C-CF3 bonds and rapid access to phenanthridine ring systems in one catalytic cycle.
- Wang, Qile,Dong, Xichang,Xiao, Tiebo,Zhou, Lei
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supporting information
p. 4846 - 4849
(2013/10/08)
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- Phenanthrene synthesis by eosin Y-catalyzed, visible light- Induced [4+2] benzannulation of biaryldiazonium salts with alkynes
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A metal-free, visible light-induced [4+2] benzannulation of biaryldiazonium salts with alkynes was developed. With eosin Y as photoredox catalyst, a variety of 9-substituted or 9,10-disubstituted phenanthrenes were obtained via a cascade radical addition and cyclization sequence. Copyright
- Xiao, Tiebo,Dong, Xichang,Tang, Yanchi,Zhou, Lei
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supporting information
p. 3195 - 3199
(2013/01/16)
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- Free-amine-directed alkenylation of C(sp2)-H and cycloamination by palladium catalysis
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A new protocol for the palladium-catalyzed free-amine-directed alkenylation of C(sp2)-H bonds and cycloamination is described. Substituted biaryl-2-amines react with various alkenes, including electron-deficient alkenes, aryl alkenes and alkyl alkenes, to give the corresponding phenanthridines with exclusive regioselectivity. The use of α-branched styrenes leads to the formation of tricyclic compounds with a seven-membered amine ring. The method operates through a free-amine-directed alkenylation and a subsequent hydroamination cyclization reaction. Seven-membered cycloamination: A new protocol for the palladium-catalyzed free-amine-directed alkenylation of C(sp2)-H bonds and subsequent cycloamination is described (see scheme). Substituted biaryl-2-amines react with various alkenes to give the corresponding phenanthridines with exclusive regioselectivity. The use of α-branched styrenes leads to the formation of tricyclic compounds with a seven-membered amine ring. Copyright
- Liang, Zunjun,Ju, Long,Xie, Yongju,Huang, Lehao,Zhang, Yuhong
-
supporting information
p. 15816 - 15821
(2013/01/16)
-
- Pd-catalyzed sequential C-C and C-N bond formations for the synthesis of N-heterocycles: Exploiting protecting group-directed C-H activation under modified reaction conditions
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Easy & efficient: A Pd-catalyzed domino olefination/conjugate addition reaction of N-Ts-2-arylanilines with activated olefins has been achieved at ambient temperature under the newly defined reaction conditions. This process highlighted the directing effect of the N-protecting group in C-H activation, displayed broad substrate scope with wide functional group compatibility; thus rendering a straightforward entry to a wide variety of N-heterocycles such as dihydrophenanthridines.
- Kim, Byung Seok,Lee, Sun Young,Youn, So Won
-
supporting information; experimental part
p. 1952 - 1957
(2011/11/04)
-
- 3-AZABICYCLO [3.1.0] HEXANE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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The present invention relates to 3-azabicyclo[3.1.0]hexane derivatives, which are useful as vanilloid receptor (VR) ligands, methods of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.
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Page/Page column 63
(2009/08/16)
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- Trifluoroacetic acid-mediated facile construction of 6-substituted phenanthridines
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The trifluoroacetic acid-mediated reaction of 2-arylanilines with arylaldehydes has been developed to give a variety of 6-substituted phenanthridines. This is a very simple and convenient one-pot process for library construction.
- Youn, So Won,Bihn, Joon Hyung
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scheme or table
p. 4598 - 4601
(2009/10/11)
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- Novel Hydroxylated Aromatic Compounds
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Pharmaceutical compositions comprising at least one compound of the formula (I) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning —X— is e.g. and Y being e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
- -
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Page/Page column 16-17
(2008/12/08)
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- First Suzuki-Miyaura type cross-coupling of ortho-azidobromobenzene with arylboronic acids and its application to the synthesis of fused aromatic indole-heterocycles
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A short synthesis of some fused indole-heterocycles has been achieved via Pd-catalyzed cross-coupling reactions between azido-2-bromobenzene and arylboronic acids and subsequent thermally induced nitrene insertion. Additionally, 4-amino-α-carboline, a versatile intermediate toward grossularine analogs has also been prepared by Suzuki-Miyaura cross-coupling of 4-pivaloylaminopyridine-3-boronic acid with 2-bromoaniline, followed by simple functional group transformations.
- Pudlo, Marc,Csányi, Dorottya,Moreau, Fabien,Hajós, Gy?rgy,Riedl, Zsuzsanna,Sapi, Janos
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p. 10320 - 10329
(2008/02/13)
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- NOVEL PHLOROGLUCINOL DERIVATIVES HAVING SELECTIN LIGAND ACTIVITY
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Pharmaceutical compositions comprising at least one compound of the formula (I) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning -X- is e.g. and Y being e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
- -
-
Page/Page column 42
(2010/11/26)
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- Imidazoline derivatives as alpha-1A adrenoceptor ligands
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Compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof are disclosed. Such compounds are useful in the treatment of Alpha-1A mediated diseases or conditions such as urinary incontinence.
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Page/Page column 29
(2010/02/11)
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- 2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.
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A series of 2'-heteroaryl and 2'-oxime anilinomethylimidazolines was prepared and evaluated in in vitro functional assays for cloned human alpha1A, alpha1B, and alpha1D receptor subtypes. Potent and selective alpha1A agonists have been identified in these series.
- Navas 3rd., Frank,Bishop, Michael J,Garrison, Deanna T,Hodson, Stephen J,Speake, Jason D,Bigham, Eric C,Drewry, David H,Saussy, David L,Liacos, James H,Irving, Paul E,Gobel, M Jeffrey
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p. 575 - 579
(2007/10/03)
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- INTRAMOLECULAR DIAZO COUPLING OF 2-AMINOPHENYLTHIOPHENES. THE FORMATION OF ISOMERIC THIENOCINNOLINES
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Thieno- (4) and thieno-cinnolines (7) have been obtained by diazotisation and internal coupling of the corresponding 2-(o-aminophenyl)thiophenes.By the same reaction 3-(o-aminophenyl)-2,5-dimethylthiophene gives 1,3-dimethylthienolcinnoline (9).
- Barton, John W.,Lapham, David J.,Rowe, David J.
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p. 131 - 134
(2007/10/02)
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