Category: 52537-00-5

On February 16, 2018, Huang, Honggui; Yu, Menglin; Su, Xiaolong; Guo, Peng; Zhao, Jia; Zhou, Jiabing; Li, Yi published an article.Application of 52537-00-5 The title of the article was Sustainable Radical Cascades to Synthesize Difluoroalkylated Pyrrolo[1,2-a]indoles. And the article contained the following:

We disclose herein a photocatalytic difluoroalkylation and cyclization cascade reaction of N-(but-2-enoyl)indoles with broad substrate scopes in up to 90% isolated yield. This method provides sustainable and efficient access to synthesize difluoroalkylated pyrrolo[1,2-a]indoles with a quaternary carbon center under mild conditions. 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 fluoroalkylated pyrroloindole synthesis photocatalytic fluoroalkylation cyclization cascade butenoylindole, radical cascade fluoroalkylated pyrroloindole synthesis, 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

Kim, Minyoung; Kumar Mishra, Neeraj; Park, Jihye; Han, Sangil; Shin, Youngmi; Sharma, Satyasheel; Lee, Youngil; Lee, Eui-Kyung; Kwak, Jong Hwan; Kim, In Su published an article in 2014, the title of the article was Decarboxylative acylation of indolines with α-keto acids under palladium catalysis: a facile strategy for the synthesis of 7-substituted indoles.COA of Formula: C8H8ClN And the article contains the following content:

Palladium-catalyzed decarboxylative acylation of highly substituted indolines with α-keto acids via C-H bond activation is described. This protocol provides efficient access to C7-carbonylated indoles, e.g., I, known to have diverse biol. profiles. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).COA of Formula: C8H8ClN

The Article related to indoline keto acid palladium decarboxylative acylation catalyst, acylated indoline preparation oxidation, indole acylated preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C8H8ClN

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

On October 28, 2010, Kawano, Tomoaki; Yonetoku, Yasuhiro; Hanazawa, Takeshi; Nigawara, Takahiro; Fukudome, Hiroki; Moritani, Hiroshi published a patent.Category: indole-building-block The title of the patent was Preparation of diacylethylenediamine compounds as DGAT1 inhibitors. And the patent contained the following:

Title compounds I [A = (un)substituted aryl, (un)substituted cycloalkyl, (un)substituted heteroaryl, etc.; ring B1 = phenylene, pyridinediyl, naphthalenediyl, etc. (herein phenylene, pyridinediyl and naphthalenediyl are optionally substituted with hydroxy, alkyl, halo, etc.); W = -O-, bond, -NH-, etc.; ring B2 = cyclohexanediyl, cyclopentanediyl or bridged ring (herein cyclohexanediyl, cyclopentanediyl and bridged ring are optionally substituted with alkyl); Y = bond, alkylene or -O-alkylene; Z = -CO2H [or biol. equivalent group thereof], carbamoyl (optionally substituted with Ph or benzyl), -OH, etc.] or salts thereof were prepared For example, reaction of Et trans-4-hydroxycyclohexanecarboxylate with benzyl 4-hydroxybenzoate in the presence of 1,1′-(azodicarbonyl)dipiperidine followed by debenzylation, EDCI-mediated amidation with tert-Bu (2-aminoethyl)carbamate, treatment with HCl, carbamoylation with trans-2-phenylcyclopropyl isocyanate, and hydrolysis afforded compound II [R = trans-2-phenylcyclopropylamino; X = H]. In diacylglycerol acyltransferase 1 (DGAT1) inhibition assays, compound II [R = 5-fluorobenzothien-2-yl; X = F] showed IC50 of 0.1 nM. Compounds I are claimed useful for the treatment of obesity. 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 diacylethylenediamine preparation dgat1 inhibitor, obesity treatment diacylethylenediamine dgat1 inhibition, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters 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 April 17, 2002, Peglion, Jean-Louis; Vilaine, Jean-Paul; Villeneuve, Nicole; Thollon, Catherine; Bourguignon, Marie-Pierre; Poitevin, Christophe published a patent.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Preparation of heterocyclic moiety-containing cyclobutenedione derivatives for use in the treatment of atherosclerosis. And the patent contained the following:

The title compounds are prepared [e.g., 3-(2,3-dihydro-1H-indol-1-yl)-4-[2-[4-(phenoxymethyl)-1-piperidinyl]ethylamino]-3-cyclobutene-1,2-dione methanesulfonate; m.p. 209-213°], along with a pharmaceutical dosage form containing them, and are useful in the treatment of diseases pertaining to endothelial dysfunction (e.g., atherosclerosis). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole

The Article related to dihydroindolylphenoxymethylpiperidinylethylaminocyclobutenedione methanesulfonate preparation antiatherosclerotic, cyclobutenedione derivative preparation antiatherosclerotic and other aspects.Application In Synthesis 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 March 4, 2004, Thorarensen, Atli; Ruble, Craig J.; Romero, Donna L. published a patent.Quality Control of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Preparation of aminoarylbenzoic acid derivatives as antibacterial agents for use as disinfectants and therapeutic agents. And the patent contained the following:

The title compounds I [X = NH; Y = CO, CS, C=NCN, or X and Y together form an alkene, or cycloalkyl; R1 = CO2H; R2 = electron withdrawing group; R4 = (un)substituted aryl with provisions] and their pharmaceutically acceptable salts are prepared and disclosed as antibacterial agents. Thus, e.g., II was prepared by conversion of 4-(chlorosulfonyl)benzoic acid to the acid chloride then amidated with Me 2-amino-5-bromobenzoate with subsequent reaction with di-Et amine and hydrolysis to give the benzoic acid moiety. In assays, the min. inhibitory concentration values (μg/mL) ranged from 0.125 – >128. As antibacterial agents I are useful for sterilization, sanitation, antisepsis, and disinfection. Claims for therapeutic use of I as an antibacterial agent are made. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Quality Control of 6-Chloro-2,3-dihydro-1H-indole

The Article related to benzoic acid aminoaryl preparation antibacterial agent antisepsis disinfection, aminoarylbenzoic acid preparation antibacterial agent sterilization sanitation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Carboxylic Acids and Peroxycarboxylic Acids and Their Sulfur-Containing Analogs and Salts and other aspects.Quality Control 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 20, 2010, Shipps, Gerald W., Jr.; Cheng, Cliff C.; Huang, Xiaohua; Achab, Abdelghani Abe; Orth, Peter; Voigt, Johannes H.; Soucy, Kyle Ann published a patent.Reference of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Preparation of aryldihydrotriazolopyrimidinone derivatives and analogs for use as fatty acid binding protein (FABP) inhibitors. And the patent contained the following:

Title compounds I [G = CR6; X = S, O, NH, etc.; or when X is CR7 or N, then X and G or X and ring Y together form a cycloalkyl or heterocyclyl ring containing 1 to 3 heteroatoms selected from N, O, or S; ring Y = (un)substituted aryl, heteroaryl, heterocyclyl, or cycloalkyl; Z = H, (un)substituted alkyl, cycloalkyl, aryl, etc.; R1 = H, alkyl, haloalkyl, haloalkoxy, etc.; each R2 independently = halo, CN, (un)substituted alkyl, etc.; R6 = absent, H, halo, (un)substituted alkyl, etc.; R7 = H, OH, (un)substituted alkoxy, or alkyl; R9 = H, halo, (un)substituted alkyl, etc.; R10 = H, halo, C(O)OH, C(O)NH2, etc.; m = 1 or 2; n = 0 to 4; with provisions], and their pharmaceutically acceptable salts, are prepared and disclosed as fatty acid binding protein (FABP) inhibitors. Thus, e.g., II was prepared by cyclization of 3-phenyl-1H-1,2,4-triazol-5-amine with Et 4-chloro-3-oxobutanoate followed by esterification with 3-chloro-2-methylphenol. I were evaluated in temperature dependence fluorescence (TdF) assays for FABP4, e.g., II demonstrated an Kd value of >0.001 to 0.5 μM. 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 triazolopyrimidinone aryldihydro derivative preparation fatty acid binding protein inhibitor, aryldihydrotriazolopyrimidinone analog preparation fatty acid binding protein fabp inhibitor 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 September 10, 2010, Kaizawa, Hiroyuki; Sugita, Mari; Azami, Hidenori; Seo, Ryushi; Nomura, Takaho; Yamamoto, Satoshi; Yamamoto, Hirofumi; Tsuchiya, Kazuyuki; Kubota, Hideki; Kamijo, Kazunori published a patent.HPLC of Formula: 52537-00-5 The title of the patent was Preparation of quinoxaline compounds as PDE9 inhibitors. And the patent contained the following:

Title compounds I [one A1 and A2 is N, the other is CR6 or N; one of R1 and R2 is H, halo, (un)substituted alkyl, etc., the other is -CONRaRb; R3 = (un)substituted alkyl, cycloalkyl, cycloalkenyl, etc.; R4, R5 = H or alkyl; R6 = H or alkyl; Ra, Rb = H, (un)substituted alkyl, cycloalkyl, etc.] or salts thereof were prepared For example, reaction of 3-chloro-2-hydrazino-7-methylquinoxaline-6-carboxylic acid Me ester with 3-chloro-4-hydroxybenzaldehyde in the presence of Cu(OAc)2 followed by hydrolysis and EDCI-mediated amidation with 1-pyridin-4-yl-1,2,3,4-tetrahydroisoquinoline afforded compound II. In PDE9 inhibition assays, IC50 of II was 2.3 nM. Compounds I are claimed useful for the treatment of urine collection disorder, urination disorder, etc. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).HPLC of Formula: 52537-00-5

The Article related to quinoxaline preparation pde9 inhibitor, urine collection disorder treatment quinoxaline preparation pde9 inhibition, urination disorder treatment quinoxaline preparation pde9 inhibition and other aspects.HPLC of Formula: 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