Category: 52537-00-5

On February 6, 2015, Park, Jihye; Mishra, Neeraj Kumar; Sharma, Satyasheel; Han, Sangil; Shin, Youngmi; Jeong, Taejoo; Oh, Joa Sub; Kwak, Jong Hwan; Jung, Young Hoon; Kim, In Su published an article.Recommanded Product: 52537-00-5 The title of the article was Mild Rh(III)-Catalyzed C7-Allylation of Indolines with Allylic Carbonates. And the article contained the following:

The rhodium(III)-catalyzed direct allylation of indolines with allylic carbonates at room temperature is described. These transformations provide the facile and efficient construction of C7-allylated indolic scaffold I [R = Me, t-Bu, NMe2, etc; R1 = H, Me, Ph, etc.]. 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 indoline allylic carbonate allylation rhodium catalyst, allylindoline preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles 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 May 6, 2022, Maji, Milan; Borthakur, Ishani; Srivastava, Sameer; Kundu, Sabuj published an article.Electric Literature of 52537-00-5 The title of the article was Regio-Selective C3- and N-Alkylation of Indolines in Water under Air Using Alcohols. And the article contained the following:

Authors disclosed a regio-selective C-H and N-H bond functionalization of indolines using alcs. in water via tandem dehydrogenation of N-heterocycles and alcs. A diverse range of N- and C3-alkylated indolines/indoles were accessed utilizing a new cooperative iridium catalyst. The practical applicability of this methodol. was demonstrated by the preparative-scale synthesis and synthesis of a psychoactive drug, N,N-dimethyltryptamine. A catalytic cycle is proposed based on several kinetic experiments and a series of control experiments and d. functional theory calculations The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Electric Literature of 52537-00-5

The Article related to indoline regioselective functionalization alc water iridium complex, heterocycle alc dehydrogenation tandem, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Electric Literature 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

On September 18, 2003, Albaugh, Pamela Ann; Ammenn, Jochen; Burkholder, Timothy Paul; Clayton, Joshua Ryan; Conner, Scott Eugene; Cunningham, Brian Eugene; Engler, Thomas Albert; Furness, Kelly Wayne; Henry, James Robert; Li, Yihong; Malhotra, Sushant; Tebbe, Mark Joseph; Zhu, Guoxin published a patent.SDS of cas: 52537-00-5 The title of the patent was Preparation of 3-(indol-3-yl) 4-heteroaryl substituted pyrrole-2,5-diones as GSK-3β inhibitors. And the patent contained the following:

The title compounds [I; Ar = (un)substituted benzofuryl, indolyl, quinolinyl, etc.; R1 = H, alkoxy, halo, etc.; R2 = H, alkyl, (un)substituted piperidin-4(or 3)-yl, etc.; R3 = H, halo, alkyl, cyclopropyl; or R2 and R3 taken together = CH2CH2CH(CH2OH)CH2; R4, R5 = H, halo], useful for treating GSK-3β mediated diseases such as diabetes and Alzheimer’s disease, were prepared Thus, reacting 2-[1-(3-hydroxypropyl)-1H-indol-3-yl]acetamide with Me (1-methyl-1H-indol-4-yl)oxoacetate in the presence of tert-BuOK in DMF afforded 54% I [Ar = 1-methyl-1H-indol-4-yl; R1, R3-R5 = H; R2 = 3-hydroxypropyl] which showed IC50 of 0.1757 μM against GSK-3β. Pharmaceutical composition comprising the compound I was claimed. 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 indolyl heteroaryl pyrroledione preparation gsk3beta inhibitor antidiabetic alzheimer’s disease, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles 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

Bakke, Jan published an article in 1974, the title of the article was New syntheses of substituted indoles.Application of 52537-00-5 And the article contains the following content:

The indoles I (R = H, 4-Cl, 6-Cl, 4-NH2) were prepd by cyclizing RC6H3(CH2CH2Cl)(NO2)-1,2 (R = H, 6-Cl, 4-Cl, 6-O2N) with Fe and dehydration of the resulting dehydroindole with Pd/C. o-O2NC6H4Me was condensed with PhCHO to give o-O2NC6H4CH2(O)HPh which was oxidized with concentrated HNO3 and the product cyclized by catalytic reduction to give 2-phenylindole. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application of 52537-00-5

The Article related to indole chloro phenyl, phenethyl chloride nitro cyclization, cyclization nitrophenethyl chloride, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Application 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

On January 19, 1995, Ham, Peter; Jones, Graham Elgin; Forbes, Ian Thomson published a patent.Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Indoline derivatives as 5-HT2C antagonists. And the patent contained the following:

Title compounds I and salts thereof are claimed [wherein P = Ph, quinoline, isoquinoline, or 5- or 6-membered aromatic heterocycle containing 1-3 N, O, and/or S atoms; R1 = H, C1-6 alkyl, halo, CF3, NR7R8, OR9; R7, R8, R9 = independently H, C1-6 alkyl, aryl-C1-6-alkyl; R2 = H, C1-6 alkyl; R3 = C1-6 alkyl; n = 0-3; m = 0-4; and R4 groups = independently C1-6 alkyl or haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C3-6-cycloalkyl-C1-6-alkyl, C1-6 alkylthio, C3-6 cycloalkylthio, C3-6-cycloalkyl-C1-6-alkylthio, halo, nitro, CF3, OCF3, SCF3, SO2CF3, SO2F, formyl, C2-6 alkanoyl, cyano, optionally substituted Ph or thienyl, NR7R8, CONR7R8, OR9, CO2R10; R10 = H, C1-6 alkyl]. I have 5-HT2C receptor antagonist activity, and some compounds also exhibit 5HT2B antagonist activity, making them potentially useful for treating a variety of central nervous and digestive system disorders. For example, reaction of 6-chloro-5-methylindoline [preparation given] with 3-pyridyl isocyanate [prepared from nicotinoyl azide in refluxing toluene] gave 62% title compound II. Testing of II in the Geller Seifter procedure [see WO 94/04533] showed a significant increase in punished responding at 0.5-10 mg/kg orally. Examples include 45 syntheses, 85 precursor preparations, and three formulations. I had pKi of 6.1-8.7 in an in vitro test for binding of [3H]-mesulergine to rat or human 5-HT2C clones, and selected I had ID50 of 0.6-15.9 mg/kg orally for reversal of MCPP-induced hypolocomotion in another bioassay. 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 indoline 5ht2c receptor antagonist preparation, serotoninergic receptor antagonist preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles 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

On October 11, 2017, Liu, Huan; Chen, Jian-Gang; Wang, Chao; Liu, Zhao-Tie; Li, Yang; Liu, Zhong-Wen; Xiao, Jianliang; Lu, Jian published an article.Product Details of 52537-00-5 The title of the article was Immobilization of Cyclometalated Iridium Complex onto Multiwalled Carbon Nanotubes for Dehydrogenation of Indolines in Aqueous Solution. And the article contained the following:

Increasing concerns about the potentially neg. impacts of chem. production on sustainable development of the overall environment have spurred numerous attempts to seek greener reaction mediums, recyclable catalysts, and high-efficiency procedures. Herein, a cyclometalated Ir complex with a pyrene tag was successfully immobilized onto multiwalled carbon nanotubes via π-π stacking interactions, through which an easily reusable Ir catalyst was constructed. The immobilization process was effectively monitored by using a fluorescence spectroscopy technique, and the immobilized Ir catalyst was well characterized and evaluated. It is found that the immobilized Ir catalyst exerts activity comparable to that of the corresponding homogeneous Ir catalyst for the dehydrogenation of indolines in an aqueous solution More importantly, the catalyst could be recycled seven times without obvious loss of the Ir-active center and noticeable decrease in the yield of the targeted product. Addnl., the observed slight deactivation of the catalyst during the recycle is also discussed. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Product Details of 52537-00-5

The Article related to indoline cyclometalated carbon nanotube immobilized iridium complex dehydrogenation catalyst, indole preparation green chem, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Product Details 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

On December 30, 2004, Howlett, Anthony R.; Rice, Audie; Moshinsky, Deborah; Hammarsten, Ola published a patent.Electric Literature of 52537-00-5 The title of the patent was A preparation of sulfonamide substituted indolinones, useful as inhibitors of DNA dependent protein kinase (DNA-PK). And the patent contained the following:

The invention relates to a preparation of sulfonamide substituted indolinones of formula I [wherein: R1 and R2 are independently selected from H, (un)substituted Ph, thiazolyl, or alkyl, etc.; R3, R4, and R5 are independently selected from H or alkyl], useful as inhibitors of DNA dependent protein kinase (DNA-PK). The invention relates to the field of radiosensitizing agents which are capable of enhancing radiotherapy by inhibiting DNA-PK (DNA-protein kinase). For instance, sulfonamide substituted indolinone II was prepared via condensation of pyrrole derivative III and indole derivative IV. The prepared indolinone derivative V was found to inhibit DNA-PK (IC50 = 1.6 μM). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Electric Literature of 52537-00-5

The Article related to sulfonamide indolinone preparation inhibitor dna dependent protein kinase, pyrrole carboxaldehyde indolone condensation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Electric Literature 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

On March 2, 2016, Zhong, Wenhe; Jin, Chuanfei; Zhang, Yingjun; Zhang, Ji published a patent.Reference of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Preparation of indoline derivatives for treating or preventing diseases related with 5-HT6 receptor. And the patent contained the following:

The invention relates to indoline derivatives (e.g., I), their stereoisomers, tautomers, nitrogen oxides, solvates, metabolites and pharmaceutically acceptable salts, and prodrugs thereof, processes for preparing them, pharmaceutical preparations comprising them, and their use for treating or preventing diseases related with 5-HT6 receptor. For instance, the invention compound I was prepared and gave a 5-HT6 Ki value of 57 nM. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Reference of 6-Chloro-2,3-dihydro-1H-indole

The Article related to indoline preparation hydroxytryptamine gastrointestinal antiobesity cns, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of 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

On May 17, 2012, Cheng, Clifford; Shipps, Gerald W., Jr.; Huang, Xiaohua; Huang, Ying; Shao, Ning; Rao, Ashwin; Palani, Anandan; Orth, Peter; Voigt, Johannes H.; Herr, Robert J.; Rossiter, Lana Michele; Zeng, Qi; Sun, Xianfeng published a patent.Application of 52537-00-5 The title of the patent was Preparation of heterocyclic inhibitors of fatty acid binding protein for use in therapy. And the patent contained the following:

The present invention relates to novel heterocyclic compounds of general formula I (wherein each of X, Y, and Z is C or N; R1 is H, halo, CN, etc.; R2 is OH, halo, C1-6alkyl, etc.; one of R3 and R4 is H or C1-6alkyl, and the other is, e.g., heteroaryl(Ra)3; Ra is H, halo, OH, etc.; or R3 and R4 together are part of a 4-7-membered ring) as Fatty Acid Binding Protein (“”FABP””) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity, or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. Synthetic procedures for preparing I are exemplified. Example compound II, prepared from 6,7-difluoro-3-hydroxyquinoxaline-2-carboxylic acid and racemic-2-(3-chlorobenzyl)pyrrolidine, had a TdF Kd value of 0.08 μM in an assay to demonstrate FABP inhibitory activity. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application of 52537-00-5

The Article related to heterocyclic inhibitor fatty acid binding protein preparation therapy, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application 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

On October 26, 2012, Woolford, Alison Jo-Anne; Howard, Steven; Buck, Ildiko Maria; Chessari, Gianni; Johnson, Christopher Norbert; Tamanini, Emiliano; Day, James Edward Harvey; Chiarparin, Elisabetta; Heightman, Thomas Daniel; Frederickson, Martyn; Griffiths-Jones, Charlotte Mary published a patent.Electric Literature of 52537-00-5 The title of the patent was Preparation of bicyclic heterocycles as anticancer agents. And the patent contained the following:

The invention relates to bicyclic heterocycles of formula I and tautomeric and stereochem. isomeric forms, N-oxides, pharmaceutically acceptable salts and the solvates thereof as anticancer agents; their preparation and use in the treatment of cancer. Compounds of formula I wherein ring E is a 6-membered aromatic carbocyclyl and heterocyclyl; G and J are independently C and N; Q is CR and N; R1 is (un)substituted C1-4 alkyl, C2-4 alkenyl and C3-8 cycloalkyl; R2 and R4 are independently (un)substituted H, C1-6 alkyl, C2-6 alkenyl, etc.; R2 and R4 together with the carbon attached form 3- to 10-membered saturated carbocyclyl and heterocyclyl; R3 and R10 are independently (un)substituted H, C1-6 alkyl, C2-6 alkenyl, etc.; R2 and R4 together with the carbon attached form 3- to 10-membered saturated carbocyclyl and heterocyclyl; R is (un)substituted C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl, etc.; and tautomeric and stereochem. isomeric forms, N-oxides, pharmaceutically acceptable salts and the solvates thereof, are claimed. Example compound II was prepared by BOC-deprotection of (R)-2-methyl-4-[2-6-methylsulfamoyl-2,3-dihydroindol-1-yl)-2-oxo-ethyl]piperazine-1-carboxylic acid tert-Bu ester. All the invention compounds were evaluated for their antiproliferative activity (some data given). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Electric Literature of 52537-00-5

The Article related to bicyclic heterocycle preparation anticancer agent, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Electric Literature 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