- NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND COMPOSITION THEREOF, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF
-
Disclosed by the present invention are a nitrogen-containing heterocyclic compound, and a composition thereof, a preparation method therefor and an application thereof. The structure of the nitrogen-containing heterocyclic compound according to the presen
- -
-
Paragraph 0318-0319
(2021/10/07)
-
- MODULATORS OF MAS-RELATED G-PROTEIN RECEPTOR X4 AND RELATED PRODUCTS AND METHODS
-
Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): (I) or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q1, Q2, Z, R, R1, R2, R3, R4 and R5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.
- -
-
Page/Page column 131-132
(2020/10/18)
-
- Fluorescent macrocyclic chemosensor for Zn(II) detection at alkaline pH values
-
The new macrocyclic ligand L (28,29-dimethoxy-27-oxa-8,11,14,17,25,26-hexaazatetracyclo[22.2.1.1(2,6).1(19,23)]nonacosa-2,4,6(28),19,21,23(29),24,26(1)-octaene) has been synthesised. It contains a tetramine chain and the 2,5-bis(2-methoxy-3-metyl-phenyl)-
- Ambrosi, Gianluca,Formica, Mauro,Fusi, Vieri,Giorgi, Luca,Micheloni, Mauro,Paderni, Daniele
-
-
- Isobenzofurans as Synthetic Intermediates: Synthesis and Biological Activity of 8-epi-(–)-Ajudazol B
-
Ajudazol B is a polyketide secondary metabolite, isolated from the myxobacterium Chondromyces crocatus, that exhibits potent biological activity. Herein, we report a convergent total synthesis of 8-epi-(–)-ajudazol B. The key step is a regio-selective alk
- Adair, Liam,Egan, Ben A.,Pearson, Colin M.,Lopez-Gonzalez, Ricardo,Kuchar, Michal,Mendoza-Mendoza, Artemio,Prunet, Jo?lle,Marquez, Rodolfo
-
supporting information
p. 6661 - 6672
(2020/10/15)
-
- Synthesis of Novel Hydroxymethyl-Substituted Fused Heterocycles
-
Examples of hydroxymethylated analogues of heteroaryl cores such as quinazolin-4-ones, isoquinolin-1(2H)-ones, pyrido[3,4-d]pyrimidin-4(3H)-ones, chromen-4-ones and pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones are sparse or non-existent in the scientific literature. We have demonstrated that such compounds are accessible by using standard procedures from readily available raw materials.
- Holmes, Jane L.,Almeida, Lynsie,Barlaam, Bernard,Croft, Rosemary A.,Dishington, Allan P.,Gingipalli, Laksmaiah,Hassall, Lorraine A.,Hawkins, Janet L.,Ioannidis, Stephanos,Johannes, Jeffrey W.,McGuire, Thomas M.,Moore, Jane E.,Patel, Anil,Pike, Kurt G.,Pontz, Timothy,Wu, Xiaoyun,Wang, Tao,Zhang, Hai-Jun,Zheng, Xiaolan
-
supporting information
p. 1226 - 1234
(2016/05/19)
-
- Stereoselective Synthesis of Isochromanones by an Asymmetric Ortho-Lithiation Strategy: Synthetic Access to the Isochromanone Core of the Ajudazols
-
Full details on the design, development, and application of a highly stereoselective strategy for the synthesis of isochromanones are reported. The method is based on an asymmetric ortho lithiation with aldehyde electrophiles and utilizes the chiral memor
- Essig, Sebastian,Menche, Dirk
-
p. 1943 - 1966
(2016/03/15)
-
- Regiodivergent Iodocyclizations for the Highly Diastereoselective Synthesis of syn - And anti -Hydroxyl-Isochromanones and -Isobenzofuranones: Concise Synthesis of the Isochromanone Core of the Ajudazols
-
An efficient synthetic strategy to access hydroxyl-isochromanone and -isobenzofurans from readily available joint alkene precursors by a regiodivergent one-pot iodocyclization-substitution tandem process is reported. The cyclizations proceed with excellen
- Thiede, Sebastian,Winterscheid, Peter Maria,Hartmann, Jan,Schnakenburg, Gregor,Essig, Sebastian,Menche, Dirk
-
p. 697 - 709
(2016/03/01)
-
- Benzylic hydroxylation of aromatic compounds by P450 BM3
-
Cytochrome P450 BM3 monooxygenase from Bacillus megaterium and its variants are promising catalysts for organic synthesis. Aiming at the identification of variants for selective hydroxylation of functionalised aromatic compounds, the double mutant F87A L188C showed remarkably improved catalytic activity towards a set of tested toluene derivatives. The apparent catalytic efficiency of this variant towards the model substrate methyl 2-methoxy-3-methylbenzoate was 63.6 s-1 M-1, which is 535-fold higher compared to that of wild-type BM3. Furthermore, the double mutant selectively catalysed the benzylic hydroxylation of numerous toluene derivatives, especially in the presence of carbonyl- or carboxyl-functions that are directly attached to the aromatic ring. Preparative scale conversion resulted in efficient production of methyl 3-(hydroxymethyl)-2-methoxybenzoate (73% yield) which proved that F87A L188C is a suitable, efficient and sustainable catalyst for the introduction of benzylic hydroxyl groups in general.
- Neufeld, Katharina,Marienhagen, Jan,Schwaneberg, Ulrich,Pietruszka, Joerg
-
p. 2408 - 2421
(2013/09/12)
-
- Regiocontrolled rearrangement of isobenzofurans
-
Regioselective alkylation and oxidative rearrangement of isobenzofurans has been achieved to generate substituted 4,8- ihydroxyisochromanones in good yields and with complete regiocontrol.
- Egan, Ben A.,Paradowski, Michael,Thomas, Lynne H.,Marquez, Rodolfo
-
supporting information; experimental part
p. 2086 - 2089
(2011/06/25)
-
- Synthesis and application of oxadiazines as chiral ligands for the enantioselective addition of diethylzinc to aldehydes
-
A series of oxadiazines derived from l-phenylalanine bearing phenolic substituents have been synthesized in a multistep, one pot process. This process involves the reaction of a mixed anhydride with a β-hydrazino alcohol, methanesulfonylation of the alcohol moiety, and base induced cyclization. The resultant oxadiazines were employed in the asymmetric addition of diethylzinc to aldehydes.
- Dean, Melissa A.,Hitchcock, Shawn R.
-
experimental part
p. 2471 - 2478
(2011/02/22)
-
- Design, synthesis and identification of novel colchicine-derived immunosuppressant
-
Synthesis and biological evaluation of various colchicine analogues through the mixed-lymphocyte reaction (MLR), lymphoproliferation, and inhibitory effects on the inflammatory genes are described. In addition, a new series of immunosuppressive agents developed on the structural basis of colchicine, as well as their structure-activity relationships is reported. The most potent analogue 20a exhibited an excellent immunosuppressive activity on in vivo skin-allograft model, which is comparable to that of cyclosporin A.
- Chang, Dong-Jo,Yoon, Eun-Young,Lee, Geon-Bong,Kim, Soon-Ok,Kim, Wan-Joo,Kim, Young-Myeong,Jung, Jong-Wha,An, Hongchan,Suh, Young-Ger
-
scheme or table
p. 4416 - 4420
(2010/04/05)
-
- A [cyclentetrakis(methylene)]tetrakis[2-hydroxybenzamide] ligand that complexes and sensitizes lanthanide(III) ions
-
The synthesis of the cyclen derivative H4L1·2 HBr containing four 2-hydroxybenzamide groups is described. The spectroscopic properties of the LnIII conplexes of L1 (Ln = Gd, Tb, Yb, and Eu) reveal changes of the
- D'Aleo, Anthony,Xu, Jide,Do, King,Muller, Gilles,Raymond, Kenneth N.
-
experimental part
p. 2439 - 2460
(2010/03/25)
-
- ARYL FLUOROETHYL UREAS ACTING AS ALPHA 2 ADRENERGIC AGENTS
-
The invention provides well-defined aryl fluoroethyl ureas that are useful as selective alpha2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of alpha2 adrenergic receptors.
- -
-
-
- LUMINESCENT MACROCYCLIC LANTHANIDE COMPLEXES
-
The present invention provides a novel class of macrocyclic compounds as well as complexes formed between a metal (e.g., lanthanide) ion and the compounds of the invention. Preferred complexes exhibit high stability as well as high quantum yields of lanthanide ion luminescence in aqueous media without the need for secondary activating agents. Preferred compounds incorporate hydroxy-isophthalamide moieties within their macrocyclic structure and are characterized by surprisingly low, non-specific binding to a variety of polypeptides such as antibodies and proteins as well as high kinetic stability. These characteristics distinguish them from known, open-structured ligands.
- -
-
Page/Page column 73
(2008/12/05)
-
- Polymer-supported O-alkylisoureas: Useful reagents for the O-alkylation of carboxylic acids
-
Polymer-supported O-alkylisoureas were prepared by reaction of an alcohol with a polymer-supported carbodiimide under copper(II) catalysis. These reagents were used to transform carboxylic acids into the corresponding methyl, benzyl, allyl, and p-nitrobenzyl esters in a highly chemoselective manner in high yields and in very high purity after simple resin filtration and solvent evaporation. The reactions could be carried out using both conventional or microwave heating, with reaction times as short as 3-5 min in the latter case, without compromising yield, purity, or chemoselectivity. Unfortunately, the corresponding solid-supported tert-butyl isoureas could not be prepared.
- Crosignani, Stefano,White, Peter D.,Linclau, Bruno
-
p. 5897 - 5905
(2007/10/03)
-
- Polymer-supported O-methylisourea: A new reagent for the O-methylation of carboxylic acids
-
(equation presented) A solid-supported O-methylisourea reagent has been prepared in one step starting from commercially available solid-supported carbodiimide. The isourea reagent has been successfully used for the preparation of methyl esters from the corresponding carboxylic acids. The crude products obtained after resin filtration and solvent evaporation are generally obtained in >98% purity.
- Crosignani, Stefano,White, Peter D.,Linclau, Bruno
-
p. 1035 - 1037
(2007/10/03)
-
- Salicylamide-lanthanide complexes for use as luminescent markers
-
The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one salicylamidyl moiety. Also provided are probes incorporating the salicylamidyl ligands of t
- -
-
-
- Oxidant scavengers
-
The present invention relates, in general, to a method of modulating physiological and pathological processes and, in particular, to a method of modulating intra- and extracellular levels of oxidants and thereby processes in which such oxidants are a participant. The invention also relates to compounds and compositions suitable for use in such methods.
- -
-
-
- The effect of an alkoxy group on the kinetic and thermodynamic acidity of benzene and toluene
-
2-, 3- and 4-Methoxytoluene can be selectively metalated at an O-adjacent ortho position when butyllithium or tert-butyllithium in the presence of sodium (potassium) tert-butoxide or N,N,N',N'',N''-pentamethyldiethylenetriamine are employed as reagents. In contrast, lithium diisopropylamide or lithium 2,2,6,6-tetramethylpiperidide deprotonate the benzylic α-position of 2- and 3-methoxytoaluene exclusively and of 4-methoxytoluene preferentially. These relative reactivities can be rationalized by an interplay of transition state stabilizing and destabilizing forces (dipole matching and metal coordination vs. lone pair repulsion).
- Schlosser, Manfred,Maccaroni, Paola,Marzi, Elena
-
p. 2763 - 2770
(2007/10/03)
-
- Derivatives of 5-hydroxy-6-methyl-2-aminotetralin
-
The title compounds were designed to provide semirigid congeners of m-tyramine in which the ring position ortho to the phenolic OH is blocked to metabolic hydroxylation. A sequence leading to a key synthetic intermediate, 5-methoxy-6-methyl-2-tetralone, h
- Cannon,Koble,Long,Verimer
-
p. 750 - 754
(2007/10/02)
-