Month: November 2022

On January 2, 2020, Ma, Dawei; Ji, Yuhua; He, Weiming; Fang, Chao; Zhao, Jinlong; Wang, Kailiang; Xia, Shanghua; Li, Zheng; Li, Ying published a patent.Name: 6-Fluoro-5-nitro-1H-indole The title of the patent was Preparation of triazole derivatives as cell necrosis inhibitors for treatment of inflammatory diseases. And the patent contained the following:

Provided by the present application are cell necrosis inhibitors with general formula I [wherein X = O, S or CH2; ring m = (un)substituted 5-6 membered heteroaryl or 5-6 membered hetero-cyclo ring fused Ph group; ring B = (un)substituted 5-12 membered aryl, 5-12 membered heteroaryl or 5-12 membered heterocyclic; R = (un)substituted (C3-C12)cycloalkyl, 5-12 membered aryl group, 5-12 membered heteroaryl group, or 5-12 membered heterocyclic group; L = O, S, NH, N(CH3)2, etc.; R1 = H or (un)substituted C1-C6 alkyl; R2 = H, halogen, hydroxy, cyano, benzyl, etc.; m = 0, 1, 2 or 3; n = 1, 2 or 3] or pharmaceutically acceptable salts thereof, the preparation method and the use thereof; in particular, provided by the present application is an inhibitor of cell necrosis and/or human receptor-interacting protein 1 kinase (RIP1). For example, compound II was prepared in a multi-step synthesis. The title compounds may be used to prevent or treat diseases involving cell death or inflammation. (assay data given). The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Name: 6-Fluoro-5-nitro-1H-indole

The Article related to preparation triazole cell necrosis inhibitor treatment inflammatory disease human, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.Name: 6-Fluoro-5-nitro-1H-indole

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On January 3, 2020, Ma, Dawei; Wang, Kailiang; Xia, Shanghua; Li, Zheng; Zhao, Jinlong; Li, Ying published a patent.Category: indole-building-block The title of the patent was Preparation of triazole derivatives as cell necrosis inhibitors for treatment of inflammatory diseases. And the patent contained the following:

Provided by the present application are cell necrosis inhibitors with general formula I [wherein X = O, S or CH2; ring m = (un)substituted 5-6 membered heteroaryl or 5-6 membered hetero-cyclo ring fused Ph group; ring B = (un)substituted 5-12 membered aryl, 5-12 membered heteroaryl or 5-12 membered heterocyclic; R = (un)substituted (C3-C12)cycloalkyl, 5-12 membered aryl group, 5-12 membered heteroaryl group, or 5-12 membered heterocyclic group; L = O, S, NH, N(CH3)2, etc.; R1 = H or (un)substituted C1-C6 alkyl; R2 = H, halogen, hydroxy, cyano, benzyl, etc.; m = 0, 1, 2 or 3; n = 1, 2 or 3] or pharmaceutically acceptable salts thereof, the preparation method and the use thereof; in particular, provided by the present application is an inhibitor of cell necrosis and/or human receptor-interacting protein 1 kinase (RIP1). For example, compound II was prepared in a multi-step synthesis. The title compounds may be used to prevent or treat diseases involving cell death or inflammation. (assay data given). The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Category: indole-building-block

The Article related to preparation triazole cell necrosis inhibitor treatment inflammatory disease human, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.Category: indole-building-block

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On November 25, 2015, Meng, Xiangbao; Yang, Jun; Li, Zhongjun published a patent.Recommanded Product: 52537-00-5 The title of the patent was Preparation of 4-substituted benzene sulfonamide derivative and their application as anticancer agents. And the patent contained the following:

The invention is related to the preparation of 4-substituted benzene sulfonamide derivative and their application as anticancer agents. The invention compounds I, wherein R1 is H, halogen, etc.; R2-R5 are independently selected from H, nitro, cyano, etc.; X is -C(R6R7)-, carbonyl, O, etc.; Y is -C(R6R7)-, O, or -N(R8)-; Z is O or S; W is N or CH; M is C1-4 linear or branched alkyl or cyclopropyl; R6 R7 and R8 are each independently selected from H, C1-4 alkyl; and their pharmaceutically acceptable salts, solvates are claimed. Compound I was prepared by multi-step procedure (procedure given). The invention compounds were evaluated for their anticancer activity. From assay, it was determined that I exhibited the IC50 value of 0.029-1.187 uM against HCT116. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Recommanded Product: 52537-00-5

The Article related to preparation substituted benzene sulfonamide derivative application anticancer agents, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.Recommanded Product: 52537-00-5

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On February 2, 2018, Wu, Yong; Yi, Hong; Lei, Aiwen published an article.Category: indole-building-block The title of the article was Electrochemical Acceptorless Dehydrogenation of N-Heterocycles Utilizing TEMPO as Organo-Electrocatalyst. And the article contained the following:

Catalytic acceptorless dehydrogenation (CAD) was a basically important organic transformation to ubiquitous unsaturated compounds without the usage of a sacrificial H acceptor. The authors successfully developed the 1st electrochem. acceptorless dehydrogenation (ECAD) of N-heterocycles using TEMPO as the organo-electrocatalyst. The authors have achieved the catalytic dehydrogenation of N-heterocycles in an anode and the release of H2 in a cathode using an undivided-cell system. A variety of six-membered and five-membered N-heteroarenes can be synthesized in good yields in this system. This protocol can also be used in the application of important mol. synthesis. The authors’ electrochem. strategy provides a mild and metal-free route for (hetero)aromatic compounds synthesis via the CAD strategy. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Category: indole-building-block

The Article related to electrochem acceptorless dehydrogenation nitrogen heterocycle tempo organo electrocatalyst, Electrochemistry: Electrodes, Electrode Reactions, and Electrode Potentials and other aspects.Category: indole-building-block

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On August 15, 2019, De Vylder, Anton; Lauwaert, Jeroen; Sabbe, Maarten K.; Reyniers, Marie-Francoise; De Clercq, Jeriffa; Van Der Voort, Pascal; Thybaut, Joris W. published an article.Synthetic Route of 79815-20-6 The title of the article was Rational design of nucleophilic amine sites via computational probing of steric and electronic effects. And the article contained the following:

Accessibility of the nucleophilic site in organocatalysts is essential to ensure adequate catalytic activity. Gas-phase trimethylborane (TMB) Lewis basicity and Bronsted proton basicity of several amine based organocatalysts have been calculated using the CBS-QB3 model chem. This TMB basicity scale can, as opposed to the proton basicity scale, account for steric effects encountered in the initial nucleophilic attack of the nitrogen free electron pair on a substrate. Since such a step is the first one in several amine catalyzed reactions, severe steric hindrance of the nucleophilic center would render the catalyst ineffective. Comparing the TMB basicity and proton basicity with the exptl. observed catalytic activity of both homogeneous and heterogeneously supported amine sites found in literature for the aldol reaction of acetone with 4-nitrobenzaldehyde showed that, due to the inclusion of these steric effects, the TMB basicity scale is a much better predictor of catalytic activity than the proton basicity. According to this computational Lewis basicity scale, potential steric hindrance in alternative nitrogen containing active sites was probed. This resulted in 3-propylpyrrolidine being proposed among the most promising monofunctional amine groups and 1-(methylamino)propan-2-ol among the most promising bifunctional amine-hydroxyl groups for heterogeneous aldol reaction catalysts. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Synthetic Route of 79815-20-6

The Article related to trimethylborane basicity amine organocatalyst bronsted proton basicity aldol condensation, Physical Organic Chemistry: Addition, Elimination, and Substitution Reactions and other aspects.Synthetic Route of 79815-20-6

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Zhang, Yinjun; Chen, Jialin; Chen, Changsheng; Wu, Shijin published an article in 2019, the title of the article was Isolation of a Bacillus Aryabhattai strain for the resolution of (R, S)-ethyl indoline-2-carboxylate to produce (S)-indoline-2-carboxylic acid.Reference of H-Idc-OH And the article contains the following content:

The strain screened from sludge can selectively hydrolyze (S)-Et indoline-2-carboxylate to produce (S)-indoline-2-carboxylic acid. It was identified as the Bacillus aryabhattai strain based on its morphol., metabolism, and 16S rDNA sequence anal. Glucose and yeast powder were used as the best carbon and nitrogen sources to cultured cells with an initial pH of seven. Subsequently, we optimized the key parameters for selective hydrolysis. Finally, when the substrate concentration had reached 3%, with a 35°C water bath, a pH of seven, and a speed of 600 rpm, the e.e.p value attained 96% with a 33% yield. Thus, we had developed a new method for producing (S)-indoline-2-carboxylic acid that used whole microbial cells as the biocatalyst. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Reference of H-Idc-OH

The Article related to bacillus aryabhattai esterase perindopril, Fermentation and Bioindustrial Chemistry: Pharmaceuticals (Including Nutrients) and other aspects.Reference of H-Idc-OH

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On May 7, 1998, Bromidge, Steven M.; Dabbs, Steven; Davies, David T.; Duckworth, D. Malcolm; Forbes, Ian T.; Ham, Peter; Jones, Graham E.; King, Frank D.; Saunders, Damian V.; Starr, Susannah; Thewlis, Kevin M.; Wyman, Paul A.; Blaney, Frank E.; Naylor, Christopher B.; Bailey, Fiona; Blackburn, Thomas P.; Holland, Vicky; Kennett, Guy A.; Riley, Graham J.; Wood, Martyn D. published an article.Related Products of 52537-00-5 The title of the article was Novel and Selective 5-HT2C/2B Receptor Antagonists as Potential Anxiolytic Agents: Synthesis, Quantitative Structure-Activity Relationships, and Molecular Modeling of Substituted 1-(3-Pyridylcarbamoyl)indolines. And the article contained the following:

The synthesis, biol. activity, and mol. modeling of a novel series of substituted 1-(3-pyridylcarbamoyl)indolines are reported. These compounds are isosteres of the previously published indole urea SB-206553 and illustrate the use of aromatic disubstitution as a replacement for fused five-membered rings in the context of 5-HT2C/2B receptor antagonists. By targeting a region of space previously identified as sterically allowed at the 5-HT2C receptor but disallowed at the 5-HT2A receptor, a number of compounds which are the most potent and selective 5-HT2C/2B receptor antagonists yet reported, were identified. 1-(3-Pyridylcarbamoyl)-5-methylthio-6-trifluoromethylindoline was selected on the basis of its overall biol. profile for further evaluation as a novel, potential nonsedating anxiolytic agent. A CoMFA anal. of these compounds produced a model with good predictive value and in addition good qual. agreement with both a 5-HT2C receptor model and a proposed binding mode for this class of ligands within that model. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Related Products of 52537-00-5

The Article related to pyridylcarbamoylindoline preparation 5ht receptor antagonist anxiolytic, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Related Products of 52537-00-5

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On June 15, 2015, Ferencz, Zs.; Adok-Sipiczki, M.; Hannus, I.; Sipos, P.; Palinko, I. published an article.Name: H-Idc-OH The title of the article was Structural features of intercalated CaFe-layered double hydroxides studied by X-ray diffractometry, infrared spectroscopy and computations. And the article contained the following:

The intercalation of various N-containing carboxylic acid anions into CaFe-layered double hydroxides was performed by the dehydration-rehydration method. Particular attention was paid to the effect of solvent mixture used during preparation It was found that various solvent mixtures resulted in different interlayer distances and, thus, different arrangements of the anions between the layers. The dimensions of the intercalated anions and detailed anal. of the IR spectra gave clues for the reasonable prediction of the spatial arrangements of the anions in the interlamellar space. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Name: H-Idc-OH

The Article related to calcium iron layered double hydroxide intercalation, Inorganic Chemicals and Reactions: Metal-Containing Salts and Related Metal-Containing Compounds and other aspects.Name: H-Idc-OH

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On January 31, 1982, Kaneko, Chikara; Fujii, Harue; Kawai, Shinji; Hashiba, Kazuhiko; Karasawa, Yoshio; Wakai, Masue; Hayashi, Reiko; Somei, Masanori published an article.Reference of Methyl 2-methyl-1H-indole-3-carboxylate The title of the article was Studies on the N-oxides of 蟺-deficient N-heteroaromatics. XXXVI. Studies on oxazepine derivatives. XII. Photochemical and thermal Michael reactions of alcohols with methyl 2-phenyl-3,1-benzoxazepine-5-carboxylate and its derivatives. And the article contained the following:

Irradiation (鈮?00 nm) of Me 2-phenyl-3,1-benzoxazepine-5-carboxylate in an alc. afforded Z-2-BzNHC6H4C(:COR)CO2Me (I, R = Me, Et, CHMe2, CMe3, allyl) as the major addition product. In contrast, thermal reaction of the oxazepine with a primary alc. in the presence of NEt3 led to the exclusive formation of E-I. Similar addition products were also obtained stereoselectively from 3,1-benzoxazepines having an acetyl group at the 5-position. E-I and Z-I were equilibrated photochem. and the stereochem. of the two isomers was determined by 1H-NMR. An explanation is proposed for the stereoselectivities observed in the photochem. and thermal reactions. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Reference of Methyl 2-methyl-1H-indole-3-carboxylate

The Article related to phenylbenzoxazepine carboxylate alcoholysis photochem thermal, benzoxazepinecarboxylate alcoholysis thermal photochem, benzamidophenylacrylate alkoxy isomer, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Esters, Acyl Peroxides, Acyl Halides and other aspects.Reference of Methyl 2-methyl-1H-indole-3-carboxylate

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On December 8, 2020, Shi, Zhuangzhi; Dong, Ben published a patent.Category: indole-building-block The title of the patent was Preparation method of indole compound for improving yield. And the patent contained the following:

A simple preparation method of indole compound capable of improving yield, and easy to synthesize without any addnl. reducing agent is provided. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Category: indole-building-block

The Article related to indole preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Category: indole-building-block

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles