Month: November 2022

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

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

On June 2, 2016, Davie, Rebecca Louise; Edwards, Hannah Joy; Evans, David Michael; Hodgson, Simon Teanby published a patent.Application In Synthesis of (2-Bromo-5-methoxyphenyl)methanamine The title of the patent was Preparation of N-((het)arylmethyl)heteroaryl-carboxamides compounds as plasma kallikrein inhibitors. And the patent contained the following:

The invention provides compounds of formula I, compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds Compounds of formula I wherein B is (un)substituted Ph, benzothiophenyl, benzofuranyl, benzomorpholinyl, etc.; W is C and X, Y, Z are independently C, N, O and S; R5 and R6 are independently H, alkyl, NH2, etc.; R7 is H; A is (un)substituted aryl and (un)substituted heteroaryl; are claimed. Example compound II was prepared by amidation of 3-(methoxymethyl)-1-(4-((2-oxopyridin-1(2H)-yl)methyl)benzyl)-1H-pyrazole-4-carboxylic acid with (3,5-dimethoxyphenyl)methanamine. The invention compounds were evaluated for their plasma kallikrein inhibitory activity (data given). The experimental process involved the reaction of (2-Bromo-5-methoxyphenyl)methanamine(cas: 887581-09-1).Application In Synthesis of (2-Bromo-5-methoxyphenyl)methanamine

The Article related to hetero arylmethyl heteroaryl carboxamide preparation plasma kallikrein inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Application In Synthesis of (2-Bromo-5-methoxyphenyl)methanamine

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

On August 10, 2021, Doi, Hisashi; Watanabe, Yasuyoshi; Choi, Yilong; Kida, Tatsuya; Tateishi, Ukihide; Kano, Daisuke; Mori, Shigeyuki; Mori, Yasuo; Uesugi, Motonari published a patent.Synthetic Route of 152626-77-2 The title of the patent was Preparation of thiazole and indazole derivatives for visualizing TRPA1. And the patent contained the following:

The present invention provides thiazole and indazole derivatives I and II [R1 = a substituent having a radioisotope; R2 = a substituent having a radioisotope] or their salts for visualizing TRPA1 (transient receptor potential ankyrin 1) in vivo. For example, compound III (preparation given) was reacted with [11C]methyl triflate (11CH3OTf, preparation given) to provide compound IV. According to the present invention, it is possible to provide a technol. for visualizing TRPA1 in vivo. The experimental process involved the reaction of 4-Bromo-5-methoxy-2-methylaniline(cas: 152626-77-2).Synthetic Route of 152626-77-2

The Article related to thiazole indazole derivative preparation trpa1 visualization bioimaging agent radioisotope, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Synthetic Route of 152626-77-2

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

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

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

On June 26, 2014, Rooney, Lisa; Vidal, Agnes; D’Souza, Anne-Marie; Devereux, Nick; Masick, Brian; Boissel, Valerie; West, Ryan; Head, Victoria; Stringer, Rowan; Lao, Jianmin; Petrus, Matt J.; Patapoutian, Ardem; Nash, Mark; Stoakley, Natalie; Panesar, Moh; Verkuyl, J. Martin; Schumacher, Andrew M.; Petrassi, H. Michael; Tully, David C. published an article.Computed Properties of 152626-77-2 The title of the article was Discovery, Optimization, and Biological Evaluation of 5-(2-(Trifluoromethyl)phenyl)indazoles as a Novel Class of Transient Receptor Potential A1 (TRPA1) Antagonists. And the article contained the following:

A high throughput screening campaign identified 5-(2-chlorophenyl)indazole as an antagonist of the transient receptor potential A1 (TRPA1) ion channel with IC50 = 1.23 μM. Hit to lead medicinal chem. optimization established the SAR around the indazole ring system, demonstrating that a trifluoromethyl group at the 2-position of the Ph ring in combination with various substituents at the 6-position of the indazole ring greatly contributed to improvements in vitro activity. Further lead optimization resulted in the identification of compound I, a potent and selective antagonist of TRPA1 in vitro (IC50 = 0.015 μM), which has moderate oral bioavailability in rodents and demonstrates robust activity in vivo in several rodent models of inflammatory pain. The experimental process involved the reaction of 4-Bromo-5-methoxy-2-methylaniline(cas: 152626-77-2).Computed Properties of 152626-77-2

The Article related to fluoromethylphenyl indazole transient receptor potential a1 ion channel antagonist, trpa1 antagonist discovery optimization sar analgesic, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Computed Properties of 152626-77-2

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

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

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

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

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

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

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

On May 8, 2003, Ghosh, Shomir; Patane, Michael A.; Carson, Kenneth G.; Chi, I-Cheng Shannon; Ye, Qing; Elder, Amy M.; Jenkins, Tracy J. published a patent.Synthetic Route of 66855-92-3 The title of the patent was Preparation of compounds as C-C chemokine receptor 8 antagonists, pharmaceutical compositions and use against inflammatory or viral disorders. And the patent contained the following:

The invention relates to (shown as I; variables defined below; e.g. 1-[1-(2′,6′-dichlorobiphenyl-3-ylmethyl)piperidin-4-yl]-1,3-dihydrobenzimidazol-2-one and 3-(3-phenoxybenzyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepine). Preferred compounds are antagonists of C-C chemokine receptor 8 (no data). The invention also relates to a method for treating a subject having an inflammatory disorder or viral disorder comprising administering to a subject in need thereof an effective amount of a compound of the invention. Although the methods of preparation are not claimed, hundreds of example preparations are included. For I: L = O, S, NRa, a bond, SO2, C(O), and (CR’R”)m; Ra = H, (un)substituted alkyl, alkylaryl, and cycloalkyl; a is 0 to 3; b is 0 to 3; m is 1 to 8; R’ and R” = H, (un)substituted alkyl, cyano and (un)substituted alkenyl. R6, R7, R8, R9 and R10 = H, hydroxy, halogen, (un)substituted C1-C10 alkyl, (un)substituted C2-C10 alkenyl, (un)substituted C2-C10 alkynyl, (un)substituted C3-C10 cycloalkyl, (un)substituted C3-C10 cycloalkenyl, (un)substituted C3-C10 cycloalkynyl, (un)substituted C3-C10 cycloalkoxy, cyano, C1-C10 alkoxy, C2-C10 alkenyloxy, C2-C10 alkynyloxy, benzyloxy, (un)substituted amino, (un)substituted amido, O(CF3), C(O)O(R1), C(O)(R1), -SO2NR1R2, trifluoromethyl, aryl, aralkyl, heteroaryl and heteroaralkyl. R1 and R2 = H and (un)substituted alkyl; Q3 is (un)substituted alkyl; R11-R19 = H, hydroxy, halogen, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted cycloalkenyl, (un)substituted cycloalkynyl, cyano, alkoxy, alkenyloxy, alkynyloxy, benzyloxy, (un)substituted amino, (un)substituted amido, O(CF3), C(O)O(R41), -C(O)(R41), -SO2NR41R42, trifluoromethyl, aryl, aralkyl, heteroaryl and heteroaralkyl; R41 and R42 = H, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted cycloalkenyl, (un)substituted cycloalkynyl, (un)substituted amino, trifluoromethyl, aryl, aralkyl, heteroaryl and heteroaralkyl; or R41 and R42 may be linked via a C2-C8 (un)substituted alkyl or alkenyl bridge where â‰? carbons may be replaced by O, S or NR46. Q5 = -N(R20)C(O)(CR41R42)1-3-, 1-N(R20)C(O)cycloalkyl (ring size = 3-9), N(R20)C(O)-substituted azacycloalkyl; R20 and R46 = H, hydroxy, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, optionally cycloalkenyl, (un)substituted cycloalkynyl, (un)substituted amino, (un)substituted amido, -C(O)O(R41), -C(O)(R41), -SO2NR4R42, trifluoromethyl, aryl, aralkyl, heteroaryl or heteroaralkyl; and Q6 = (un)substituted aromatic ring, (un)substituted nonaromatic heterocycle, and (un)substituted heteroaromatic ring; or R18 or R19 together with Q5Q6 and the atoms to which they are bonded form an (un)substituted nonaromatic carbocyclic group, (un)substituted nonaromatic heterocyclic group, (un)substituted aryl ring or (un)substituted heteroaryl ring. Addnl. details are given in the claims. The experimental process involved the reaction of 3-(2-Methoxyphenoxy)benzaldehyde(cas: 66855-92-3).Synthetic Route of 66855-92-3

The Article related to ccr8 chemokine receptor antagonist preparation anti inflammatory antiviral agent, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Synthetic Route of 66855-92-3

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

On September 15, 2021, Siccama, Joanne W.; Pegiou, Eirini; Eijkelboom, Nienke M.; Zhang, Lu; Mumm, Roland; Hall, Robert D.; Schutyser, Maarten A. I. published an article.COA of Formula: C8H10O2 The title of the article was The effect of partial replacement of maltodextrin with vegetable fibres in spray-dried white asparagus powder on its physical and aroma properties. And the article contained the following:

Asparagus concentrate was spray-dried in different carrier formulations in which maltodextrin was partially replaced by cellulose-based carriers, i.e. asparagus fiber, citrus fiber or microcrystalline cellulose. This replacement was limited to a maximum level of 3% weight/weight for asparagus and citrus fibers, and 10% weight/weight for microcrystalline cellulose, due to fiber insolubility and increased viscosity of the feed. Powders obtained from feed solutions with an initial solids content of 40% weight/weight showed better phys. properties and aroma retention than 30% weight/weight Partial replacement of maltodextrin by cellulose-based carriers resulted in powders with similar phys. properties as the control and did not detrimentally influence the aroma profiles as analyzed by headspace solid-phase microextraction and gas chromatog.-mass spectrometry. This research shows that fiber obtained from asparagus waste streams could potentially be used as a carrier to produce spray-dried asparagus powder with retained key asparagus volatiles such as 2-methoxy-3-iso-Pr pyrazine. The experimental process involved the reaction of 1,2-Dimethoxybenzene(cas: 91-16-7).COA of Formula: C8H10O2

The Article related to maltodextrin vegetable fiber asparagus spray drying aroma, asparagus fibres, gc–ms, maltodextrin, metabolomics, spray drying, volatiles retention, Food and Feed Chemistry: Fruits, Vegetables, Legumes, and Nuts and other aspects.COA of Formula: C8H10O2

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