Tag: 100-200

On May 20, 2021, Li, Jinping; Lou, Jun; Guo, Xiaodan; Zeng, Xian; Chen, Yongkai; Zhang, Yihan; Peng, Wei; Wang, Chaodong published a patent.Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Preparation of the rock inhibitor and their medical applications. And the patent contained the following:

The invention is related to the preparation of the rock inhibitor I and their medical applications. The invention compounds I, wherein W and V are independently C or N;X is -C (=0) NRx-, -NRx-C (=O); Y is a chem. bond, or unsubstituted or optionally substituted by one, two or more Ry groups, etc.; ring A is unsubstituted or optionally substituted with one, etc.; ring B is unsubstituted or optionally substituted by one, etc.; ring C is unsubstituted or optionally substituted by one, two or more Rc groups as follows: C3_20 alicyclic hydrocarbon group, 3-20 no heterocyclic group, C6-20 aryl or 5-20 membered heteroaryl; ring D is the following group unsubstituted or optionally substituted by one, two or more Rd: C3_20 alicyclic hydrocarbon group, 3-20 membered heterocyclic group,C6_2() aryl or 5-20 membered heteroaryl; Ry, Rab, Rc, Rd are each independently selected from H, halogen, nitro, nitroso, etc.; and their racemates, stereoisomers, tautomers, isotopic markers, nitrogen oxides, solvates, polymorphs, metabolites, esters, pharmaceutically acceptable salts, or prodrugs are claimed. Compound I was prepared by multi-step procedure (procedure given). The invention compounds I were evaluated for their ROCK inhibitory activity. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole

The Article related to preparation rock inhibitor medical application, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Recommanded Product: 6-Chloro-2,3-dihydro-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

Jiang, Xue; Wang, Chao; Wei, Yawen; Xue, Dong; Liu, Zhaotie; Xiao, Jianliang published an article in 2014, the title of the article was A General Method for N-Methylation of Amines and Nitro Compounds with Dimethylsulfoxide.SDS of cas: 52537-00-5 And the article contains the following content:

DMSO reacts with a broad range of amines in the presence of formic acid, providing a novel, green and practical method for amine methylation. The protocol also allows the one-pot transformation of aromatic nitro compounds into di-Me amines in the presence of a simple iron catalyst. A mechanistic study indicated that the synthesis of the target compounds was achieved by a methylene group transfer from DMSO to an amine, formation of an imine intermediate and subsequent reduction of this imine by formic acid. A reaction of 2-[2-(1,3-benzodioxolyl)ethyl]-1,2,3,4-tetrahydroquinoline with DMSO/HCO2H gave 2-[2-(1,3-benzodioxolyl)ethyl]-1,2,3,4-tetrahydro-1-(methyl)quinoline (allocuspareine, galipinine). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).SDS of cas: 52537-00-5

The Article related to methylation alkylation amine dmso, secondary primary amine nitrobenzene methylation dmso formic acid, dmso, amines, deuterium labelling, formic acid, methylation, Alkaloids: Alkaloids Containing One Nitrogen Atom In A Ring and other aspects.SDS of cas: 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

Hsu, Shih-Fan; Ko, Chih-Wei; Wu, Yao-Ting published an article in 2011, the title of the article was Cobalt-Catalyzed Carbon-Carbon Bond Formation: Synthesis and Applications of Enantiopure Pyrrolidine Derivatives[1] [Erratum to document cited in CA155:241131].COA of Formula: C9H9NO2 And the article contains the following content:

On page 1762, stereochem. was omitted from Reference 27; the correction is given. The graphical abstracted contained a capitalization error; the corrected abstract is given. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).COA of Formula: C9H9NO2

The Article related to erratum pyrrolidine enantiopure preparation cross coupling cobalt catalyzed, tylophorine synthesis cross coupling cobalt catalyzed erratum, Alkaloids: Alkaloids Containing One Nitrogen Atom In A Ring and other aspects.COA of Formula: C9H9NO2

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 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

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 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 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 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 December 16, 2015, Liu, Zhaotie; Liu, Huan; Wang, Chao; Chen, Jiangang; Liu, Zhongwen; Xiao, Jianliang published a patent.Synthetic Route of 52537-00-5 The title of the patent was A recyclable supported cyclic metal iridium catalyst and its preparation method and application in dehydrogenation reaction of indoline series compound. And the patent contained the following:

The present invention discloses a recyclable supported cyclic metal iridium catalyst and its preparation method and application in dehydrogenation reaction of indoline series compound The catalyst is pyrene-labeled cyclic metal iridium complex, which uses multi-walled carbon nanotubes as carrier. The pyrene-labeled cyclic metal iridium complex has structural formula as in Claim 1. The cyclic metal iridium complex uses iridium atom as coordination center, uses 4-methoxy-N-[1-(4- hydroxyphenyl)methylene]-aniline and pentamethyl cyclopentadiene as ligand. The preparation method includes: synthesis of 4-methoxy-N-(1-(4-hydroxyphenyl)methylene)-aniline; (2) synthesis of cyclic metal iridium complex; (3) synthesis of pyrene-labeled cyclic metal iridium complex; (5) preparation of the supported cyclic metal iridium catalyst. The inventive catalyst has simple preparation method, short preparation period, can achieve dehydrogenation reaction of indoline series compound in green solvent (mixed solvent of water and trifluoroethanol); the reaction conditions are mild, safe, green and efficient. The inventive catalyst can be recycled through simple centrifuge separation, and can keep its excellent catalytic performance after reused many times. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Synthetic Route of 52537-00-5

The Article related to recyclable supported cyclic metal iridium catalyst dehydrogenation indoline, Catalysis, Reaction Kinetics, and Inorganic Reaction Mechanisms: Catalysts and other aspects.Synthetic Route of 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