Tag: 100-200

On June 25, 2009, Chen, Li; Dillon, Michael Patrick; Feng, Lichun; Hawley, Ronald Charles; Yang, Minmin published a patent.Application of 1162054-86-5 The title of the patent was Preparation of imidazole-substituted arylamides as P2X3 and P2X2/3 antagonists for disease treatment. And the patent contained the following:

Compounds of the formula I (wherein R1 is (un)substituted imidazolyl; R2 is Ph, pyridinyl, pyrimidinyl, etc., all optionally substituted; R3 is H, C1-6-alkyl, hetero-C1-6-alkyl, or CN; R4 is H, C1-6-alkyl, or hetero-C1-6-alkyl; or R3 and R4 together form part of a ring; R5 is C1-6alkyl, hetero-C1-6alkyl; halo-C1-6alkyl, etc.; or R3, R4, and R5 together form part of a ring; and R6, R7 and R8 are independently H, C1-6-alkyl, C1-6-alkyloxy, halo, C1-6-haloalkyl, or CN) are provided herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds More particularly I are usable for treatment of genitourinary, pain, inflammatory, gastrointestinal and respiratory diseases, conditions and disorders. Example compound II was prepared by reacting imidazole with the appropriate 5-iodobiphenylcarboxamide intermediate. In a P2X3 FLIPR (fluorometric imaging plate reader) assay, example compound III had a pIC50 of approx. 8.55 for the P2X3 receptor. The experimental process involved the reaction of (S)-1-Methoxypropan-2-amine hydrochloride(cas: 1162054-86-5).Application of 1162054-86-5

The Article related to imidazole arylamide preparation p2x3 p2x2 receptor antagonist disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Application of 1162054-86-5

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On June 18, 2021, Knorrscheidt, Anja; Soler, Jordi; Huenecke, Nicole; Puellmann, Pascal; Garcia-Borras, Marc; Weissenborn, Martin J. published an article.Quality Control of 2-Methoxynaphthalene The title of the article was Accessing chemo- and regioselective benzylic and aromatic oxidations by protein engineering of an unspecific peroxygenase. And the article contained the following:

Unspecific peroxygenases (UPOs) enable oxyfunctionalizations of a broad substrate range with unparalleled activities. Tailoring these enzymes for chemo- and regioselective transformations represents a grand challenge due to the difficulties in their heterologous productions. Herein, we performed protein engineering in Saccharomyces cerevisiae using the MthUPO from Myceliophthora thermophila. More than 5300 transformants were screened. This protein engineering led to a significant reshaping of the active site as elucidated by computational modeling. The reshaping was responsible for the increased oxyfunctionalization activity, with improved kcat/Km values of up to 16.5-fold for the model substrate 5-nitro-1,3-benzodioxole. Moreover, variants were identified with high chemo- and regioselectivities in the oxyfunctionalization of aromatic and benzylic carbons, resp. The benzylic hydroxylation was demonstrated to perform with enantioselectivities of up to 95% ee. The proposed evolutionary protocol and rationalization of the enhanced activities and selectivities acquired by MthUPO variants represent a step forward toward the use and implementation of UPOs in biocatalytic synthetic pathways of industrial interest. The experimental process involved the reaction of 2-Methoxynaphthalene(cas: 93-04-9).Quality Control of 2-Methoxynaphthalene

The Article related to saccharomyces unspecific peroxygenase protein engineering, Fermentation and Bioindustrial Chemistry: Industrial Chemicals and other aspects.Quality Control of 2-Methoxynaphthalene

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On February 16, 2017, Pourashraf, Mehrnaz; Jacquemot, Guillaume; Claridge, Stephen; Bayrakdarian, Malken; Johnstone, Shawn; Albert, Jeffrey S.; Griffin, Andrew published a patent.Safety of (S)-1-Methoxypropan-2-amine hydrochloride The title of the patent was Substituted benzimidazoles as bromodomain inhibitors, their preparation and their use as pharmaceuticals. And the patent contained the following:

This application relates to substituted benzimidazoles of formula I, compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. The application also relates to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasm. Compounds of formula I wherein R1 is (un)substituted C1-6 alkyl, COR11, CONHR11, SO2R11, etc.; R2 is H, (un)substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl etc.; R3 and R6 are independently H, (un)substituted C1-6 alkyl, COR11, NH2 and derivatives, CONH2 and derivatives, etc.; one of R4 and R5 is H, (un)substituted C1-6 alkyl, COR11, NH2 and derivatives, CONH2 and derivatives, etc., and the other one of R4 and R5 is 6-membered nitrogen containing heterocycle; R11 is (un)substituted C1-6 alkyl;and pharmaceutically acceptable salts, solvates, esters and prodrugs thereof, are claimed. Example compound II was prepared by amidation of tetrahydropyran-4-carbonyl chloride with 4-bromo-N2-[2-(trifluoromethoxy)ethyl]benzene-1,2-diamine followed by cyclization; the resulting 6-bromo-2-tetrahydropyran-4-yl-1-[2-(trifluoromethoxy)ethyl]benzimidazole underwent cross-coupling reaction with 1,3-dimethyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-one to give compound II. The invention compounds were evaluated for their bromodomain inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 0.076 μM to 0.14 μM. The experimental process involved the reaction of (S)-1-Methoxypropan-2-amine hydrochloride(cas: 1162054-86-5).Safety of (S)-1-Methoxypropan-2-amine hydrochloride

The Article related to benzimidazole preparation bromodomain inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Safety of (S)-1-Methoxypropan-2-amine hydrochloride

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Zhou, Jun; Mao, Lijun; Wu, Meng-Xiang; Peng, Zhiyong; Yang, Yiming; Zhou, Manfei; Zhao, Xiao-Li; Shi, Xueliang; Yang, Hai-Bo published an article in 2022, the title of the article was Extended phenothiazines: synthesis, photophysical and redox properties, and efficient photocatalytic oxidative coupling of amines.Application of 93-04-9 And the article contains the following content:

Herein authors successfully developed a ring-fusion approach to extend the conjugation length of phenothiazines and synthesized a series of novel extended phenothiazines. The intriguing π-conjugation length-dependent photophys. and redox properties of these extended phenothiazines, and their photocatalytic performance towards visible-light-driven oxidative coupling reactions of amines were systematically investigated. As compared with the conventional phenothiazine (PTZ), all the extended phenothiazines displayed reversible redox behavior and maintained a strong excited-state reduction potential as well. Consequently, phenothiazines with longer effective conjugation lengths could efficiently catalyze the oxidative coupling of amines to imines under visible-light irradiation; by comparison, the shorter PTZ could only catalyze such reactions in the presence of UV light. Moreover, one PTZ showed superior catalytic performance which can result in better yields within a shorter reaction time, and in a broad substrate scope. Finally, a direct and efficient conversion of amines to imines under sunlight in an air atm. was successfully realized. Authors believe that their study including the new phenothiazine modification methodol. and the newly developed extended phenothiazine-based photocatalysts will open up a new way to develop novel phenothiazine-based materials for optoelectronic and catalytic applications. The experimental process involved the reaction of 2-Methoxynaphthalene(cas: 93-04-9).Application of 93-04-9

The Article related to extended phenothiazine preparation photophys redox property, imine preparation, amine photocatalytic oxidative coupling phenothiazine, Heterocyclic Compounds (More Than One Hetero Atom): Thiazines and other aspects.Application of 93-04-9

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On April 13, 2021, Liao, Qingyu; Chen, Dong; Zhang, Xianhong; Ma, Yuhong; Zhao, Changwen; Yang, Wantai published an article.COA of Formula: C6H12O3 The title of the article was UV-Assisted Li+-Catalyzed Radical Grafting Polymerization of Vinyl Ethers: A New Strategy for Creating Hydrolysis-Resistant and Long-Lived Polymer Brushes as a “Smart” Surface Coating. And the article contained the following:

A facile synthetic route was developed to prepare a surface-grafted brush layer of poly(vinyl ethers) (PVEs) directly by a radical mechanism, with the “naked” Li+ acting as a catalyst. D. functional theory calculations suggested that complexation of naked Li+ to VEs significantly reduced the highest unoccupied MO-LUMO (HOMO-LUMO) energy gap from 5.08 to 0.68 eV, providing a better prospect for electron transfer. The structure, morphol., and surface properties of grafted polymer layers were characterized using attenuated total reflection Fourier transform IR spectroscopy, Raman spectroscopy, XPS, at. force microscopy, and dynamic water contact angle (DCA). Moreover, ellipsometry data indicated that the thickness of the polymer brushes was in the range of 20-60 nm, which corresponds to the grafting densities of 0.65-1.15 chain/nm2, and DCA decreased from 84.4 to 45.3°. Most importantly, no hydrolysis was observed for the modified surface after 30 days of exposure to phosphate-buffered saline solution, 0.1 mol/L NaOH(eq) and 0.1 mol/L HCl(eq), demonstrating excellent hydrolysis resistance with long service life. In addition, as a proof of concept, the side hydroxyl groups of grafted PVEs provide active sites for efficient fixation of bioactive mols., e.g., glycosaminoglycan and serum protein. The experimental process involved the reaction of 2-(2-(Vinyloxy)ethoxy)ethanol(cas: 929-37-3).COA of Formula: C6H12O3

The Article related to uv assisted li catalyzed radical grafting polymerization vinyl ether, Coatings, Inks, and Related Products: Other Coating Materials and other aspects.COA of Formula: C6H12O3

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Ether – Wikipedia,
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On July 27, 2020, Deichert, Julie A.; Mizufune, Hideya; Patel, Jignesh J.; Hurst, Timothy E.; Maheta, Ashish; Kitching, Mathew O.; Ross, Avena C.; Snieckus, Victor published an article.Synthetic Route of 321-28-8 The title of the article was Expedient Pd-Catalyzed α-Arylation towards Dibenzoxepinones: Pivotal Manske’s Ketone for the Formal Synthesis of Cularine Alkaloids. And the article contained the following:

The general synthesis of diversely substituted dibenzoxepinones by a combined Pd-catalyzed α-arylation and SNAr strategy is reported and applied to the synthesis of Manske’s ketone, a key intermediate en route to the total synthesis of cularine alkaloids. In the course of this work, an unanticipated ring contraction reaction to a xanthone was observed and serves as a caveat for the conditions of the widely used α-arylation reaction. Thus, e.g., o-(2-bromophenoxy)acetophenone â†?dibenzoxepinone I (72%) in presence of Pd2(dba)3 and XantPhos, Cs2CO3 as base and toluene as solvent. The experimental process involved the reaction of 1-Fluoro-2-methoxybenzene(cas: 321-28-8).Synthetic Route of 321-28-8

The Article related to palladium catalyzed arylation benzoxepinone manske ketone synthesis, cularine alkaloid formal synthesis, Alkaloids: Alkaloids Containing One Nitrogen Atom In A Ring and other aspects.Synthetic Route of 321-28-8

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On February 29, 2020, Hassine, Manel; Ben Jannet, Hichem; Ghermani, NourEddine; Alami, Mouad; Messaoudi, Samir published an article.Reference of 1-Fluoro-2-methoxybenzene The title of the article was Synthesis of N-(Hetero)arylconvolvine Derivatives through a Palladium-Catalyzed Buchwald-Hartwig Cross-Coupling. And the article contained the following:

The present study describes the isolation of convolvine from the roots of the Tunisian plant Convolvulus dorycnium L. and its synthesis through a four-step sequence starting from tropine. Then, an efficient synthesis of N-(het)aryltropanes derivatives by a sequence of a palladium-catalyzed N-arylation of convolvine has been established. This strategy enabled access to unknown tropane scaffolds of biol. interests. The antitumor activity of the derivatives against HCT-116 cell line was tested. The experimental process involved the reaction of 1-Fluoro-2-methoxybenzene(cas: 321-28-8).Reference of 1-Fluoro-2-methoxybenzene

The Article related to convolvine aryl derivative preparation buchwald hartwig cross coupling antitumor, Alkaloids: Alkaloids Containing One Nitrogen Atom In A Ring and other aspects.Reference of 1-Fluoro-2-methoxybenzene

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Li, Yi-Xian; Ren, Iwaki; Kato, Atsushi; Jia, Yue-Mei; Fleet, George W. J.; Zhao, Xuan; Xiao, Min; Yu, Chu-Yi published an article in 2016, the title of the article was Fluorinated Radicamine A and B: Synthesis and Glycosidase Inhibition.Computed Properties of 321-28-8 And the article contains the following content:

Fluorinated derivatives of radicamine A and radicamine B, I (R1 = F, R2 = R3 = H, R4 = OH; R1 = R3 = H, R2 = F, R4 = OH; R1 = R2 = H, R3 = F, R4 = OH; R1 = R2 = R3 = H, R4 = F) and II (R1 = F, R2 = H; R1 = H, R2 = F), resp., have been synthesized from D-arabinose-derived cyclic nitrone III. Structure-activity relationship studies showed that glycosidase inhibition of these fluorinated derivatives was significantly influenced by the position of the fluorine atom. C-7 or C-11 fluorination of the aromatic ring decreased α-glucosidase inhibition of the derivatives, whereas C-8 or C-10 fluorination preserved glycosidase inhibitory activities. The experimental process involved the reaction of 1-Fluoro-2-methoxybenzene(cas: 321-28-8).Computed Properties of 321-28-8

The Article related to radicamine a b fluorinated preparation glycosidase inhibitor structure activity, Alkaloids: Alkaloids Containing One Nitrogen Atom In A Ring and other aspects.Computed Properties of 321-28-8

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On January 31, 2015, He, Nana; Wu, Xiaoqin; Guo, Xianghai; Bai, Peng published an article.Product Details of 321-28-8 The title of the article was ortho-fluoroanisole: A new donor for boron isotopes separation by chemical exchange distillation. And the article contained the following:

10B is an effective neutron absorbent, which endows its duty in nuclear industry as a protecting agent. The only industrialized process for preparation of 10B is chem. exchange distillation using anisole as a complexing agent. The drawbacks such as low isotope separation factor and instability under process conditions inspired continuous interests to find a replacement. A new complexing agent, o-fluoroanisole, was selected and evaluated for boron isotopes separation O-fluoroanisole demonstrates better properties such as higher separation factor, lower f.p. of the complex and longer cycle life compared with those of anisole, which suggest it as a noteworthy agent used for separating isotopes. The experimental process involved the reaction of 1-Fluoro-2-methoxybenzene(cas: 321-28-8).Product Details of 321-28-8

The Article related to ortho fluoroanisole donor boron isotope separation chem exchange distillation, Nuclear Technology: Isotopes and Isotopic Radiation Sources and other aspects.Product Details of 321-28-8

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Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

On July 31, 2020, Yu, Wen-Shuai; Wu, Ze-Nong; Qiu, Zeng-Feng; Zhao, Chun-Jie; Zhang, Fu-Li; Yang, Zhe-Zhou published an article.Category: ethers-buliding-blocks The title of the article was One-Pot Synthesis of Papaverine Hydrochloride and Identification of Impurities. And the article contained the following:

A one-pot synthesis of papaverine hydrochloride with 99.6% purity was performed using xylene as solvent for the entire process. The critical parameters of each step, as well as the impurities generated, were identified. The overall yield was improved to 63%. The proposed synthetic procedure was suitable for industrial production The experimental process involved the reaction of 1,2-Dimethoxybenzene(cas: 91-16-7).Category: ethers-buliding-blocks

The Article related to papaverine hydrochloride preparation, Alkaloids: Alkaloids Containing One Nitrogen Atom In A Ring and other aspects.Category: ethers-buliding-blocks

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Ether – Wikipedia,
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