Category: 52537-00-5

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 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

On November 1, 2014, Yang, Jun; Zhou, Shanshan; Ji, Liyan; Zhang, Chao; Yu, Siwang; Li, Zhongjun; Meng, Xiangbao published an article.Name: 6-Chloro-2,3-dihydro-1H-indole The title of the article was Synthesis and structure-activity relationship of 4-azaheterocycle benzenesulfonamide derivatives as new microtubule-targeting agents. And the article contained the following:

A series of 1-sulfonyl indolines was synthesized and evaluated for antiproliferative activity. The most potent compounds I (R = H or MeO) showed significant cytotoxicity (IC50 in the range of 0.055-0.105 and 0.039-0.112 μM, resp.) against four human cancer cell lines HCT116, PC3, HepG2 and SK-OV-3. The structure-activity relationship of this series of sulfonamides, including the influence of azaheterocycle rings, substituent at the different positions of indolines, and the cyclopropane moiety, was described. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Name: 6-Chloro-2,3-dihydro-1H-indole

The Article related to indoline azaheterocycle benzenesulfonamide preparation microtubule targeting agent antitumor, benzenesulfonamides, indoline, microtubule-targeting agents, synthesis, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.Name: 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 14, 2020, Lee, Matthew Randolph; Varano, Anthony Joseph published a patent.Safety of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Sulfonylisoquinoline derivatives as Rock kinase inhibitors and their preparation. And the patent contained the following:

The invention relates to compounds of formula I as Rho-associated protein kinases (ROCK) inhibitors useful for treatment of cerebral cavernous malformation syndrome and cardiovascular diseases. Compounds of formulas I and II wherein ring X is partially saturated aza-containing heteroaryl; Y is CH or N; m is 0, 1, 2 and 3; each R1 is independently CN, OH, hydroxyalkyl, halo, etc.; R2 is H and halo; R3 is H, halo and C1-3 alkyl; with provisions; and pharmaceutically acceptable salts thereof, are claimed. Example compound III was prepared by sulfonylation of 1-chloroisoquinoline with chlorosulfonic acid; the resulting 1-chloroisoquinoline-5-sulfonyl chloride underwent hydrolysis to give 1-hydroxyisoquinoline-5-sulfonic acid, which underwent chlorination to give the corresponding sulfonyl chloride, which underwent amidation with 4-methylisoindoline to give compound III. Exemplified I were evaluated for selective ROCK kinase inhibitory activity from which III demonstrated IC50 values in the range of >1000 nM and ≤10,000 nM for both ROCK1 and ROCK2 compared to IC50 values of >10,000 for PKACA, AKT1, and PKG, resp. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Safety of 6-Chloro-2,3-dihydro-1H-indole

The Article related to sulfonylisoquinoline derivative preparation rock kinase inhibitor cavernous malformation syndrome, selective rock1 rock2 inhibitor cardiovascular disease, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Safety 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 December 15, 2011, Zhang, Hesheng; Chen, Yingwei; He, Qingchao published a patent.Safety of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Cyanoquinoline derivatives as tyrosine kinase receptor inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:

Disclosed are Cyanoquinoline derivatives compounds of formula I and their stereoisomers, cis-/trans-isomers, tautomers or mixtures thereof, or pharmaceutically acceptable salts, solvates or prodrugs thereof. Compounds of formula I, wherein R1 is (un)substituted alkylcarbonylamino, (un)substituted alkenylcarbonylamino, (un)substituted alkynylcarbonylamino, (un)substituted arylcarbonylamino, (un)substituted amino and (un)substituted alkoxy; R2 and R3 are independently H, (un)substituted arylalkyl and (un)substituted (hetero)aryl; R2R3 may be taken together with the nitrogen atom attached to form (un)substituted heterocyclyl; R4 (un)substituted heterocyclyl and (un)substituted heteroaryl; and their stereoisomers, cis-/trans-isomers, tautomers or mixtures thereof, or pharmaceutically acceptable salts, solvates or prodrugs thereof, are claimed. Compounds of formula I were prepared via nitration of Me 2-(acetylamino)-4-fluorobenzoate; the resulting Me 2-(acetylamino)-4-fluoro-5-nitrobenzoate underwent condensation with alcs. followed by decarboxylation and deacetylation to give 3-alkoxy-4-nitroanilines, which underwent condensation with Et 2-cyano-2-(ethoxymethylene)acetate to give Et 2-cyano-3-[(3-alkoxy-4-nitrophenyl)amino]acrylates, which underwent intramol. cyclization to give 7-alkoxy-3-cyano-4-hydroxy-6-nitroquinolines, which underwent chlorination to give 7-alkoxy-3-cyano-4-chloro-6-nitroquinolines, which underwent condensation with amines to give 7-alkoxy-3-cyano-4-amino-6-nitroquinolines, which underwent reduction to give 7-alkoxy-3-cyano-4,6-diaminoquinolines, which underwent N-alkylation to give I. All the invention compounds were evaluated for their tyrosine kinase receptor inhibitory activity. From the assay, it was determined that example compound I (R1 = [(E)-4-(dimethylamino)-2-butenoyl]amino, R2 = H, R3 = 3-ethynylphenyl and R4 = tetrahydrofuran-3-yl) exhibited the IC50 value of 0.024 μM with the inhibition of 85% against A431 cell lines. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Safety of 6-Chloro-2,3-dihydro-1H-indole

The Article related to cyano quinoline preparation tyrosine kinase receptor inhibitor treatment cancer, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Safety 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 7, 2013, Courtney, Stephen Martin; Prime, Michael; Mitchell, William; Brown, Christopher John; De Aguiar Pena, Paula C.; Johnson, Peter; Dominguez, Celia; Toledo-Sherman, Leticia M.; Munoz, Ignacio published a patent.Computed Properties of 52537-00-5 The title of the patent was Preparation of phenylpyrimidine derivatives and analogs for use as kynurenine-3-monooxygenase inhibitors. And the patent contained the following:

Title compounds I [L = C(O), C(O)O, C(O)NR4, NR4S(O)2, etc.; X and Y independently = N or CH, provided at least one is N; R1 = (un)substituted aryl or heteroaryl; R2 = H or alkyl; R3 = H, OH, halo, alkyl, etc.; R4 and R5 taken together with the N atom to which they are attached to form an (un)substituted heterocycloalkyl, aryl, heteroaryl, etc.; with provisions], and their pharmaceutically acceptable salts, are prepared and disclosed as kynurenine-3-monooxygenase inhibitors. Thus, e.g., II was prepared by a multistep procedure (preparation given). Select I were evaluated as kynurenine-3-monooxygenase inhibitors (data given). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Computed Properties of 52537-00-5

The Article related to pyrimidine derivative preparation kynurenine monooxygenase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties 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 3, 2013, Suzuki, Masaki; Kondo, Kazumi; Kurimura, Muneaki; Valluru, Krishna Reddy; Takahashi, Akira; Kuroda, Takeshi; Takahashi, Haruka; Fukushima, Tae; Miyamura, Shin; Ghosh, Indranath; Dogra, Abhishek; Harriman, Geraldine; Elder, Amy; Shimizu, Satoshi; Hodgetts, Kevin J.; Newcom, Jason S. published a patent.Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Quinazolines as STEP inhibitors and their preparation and use in the treatment of central nervous system agents. And the patent contained the following:

Methods of treating disorders using quinazoline compounds of formula I that modulate STriatal-enriched tyrosine phosphatase (STEP) are described herein. Compounds of formula I wherein m is 0 and 1; L is a bond and NH and derivatives; R1 is H, C1-8 alkyl, halo, C1-8 haloalkyl, etc.; R2 is C1-8 alkoxy, benzodioxolyl, piperazinyl, halo, etc.; R3 is pyridinyl, pyrimidinyl, pyrazinyl, etc.; R4 is H, C1-8 alkyl, C1-8 alkoxy, etc.; and salts thereof, are claimed. Example compound II•3HCl was prepared by amination of 4-bromo-6-methoxy-2-(pyridin-3-yl)quinazoline with 3-aminopyridine-2-carboxamide. All the invention compounds were evaluated for their STEP inhibitory activity (some data given). 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 quinazoline preparation step inhibitor treatment cns disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines 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 December 10, 2002, Munchhof, Michael John; Sobolov-Jaynes, Susan Beth; Marx, Matthew Arnold published a patent.Related Products of 52537-00-5 The title of the patent was Preparation of thienopyrimidines and thienopyridines as anticancer agents. And the patent contained the following:

The title compounds [I and II; X1 = CH; R1 = H, alkyl, C(O)alkyl; R2 = aryl, heterocyclic; R11 = H, alkyl, C(O)NR6R9, etc.; R6 = H, alkyl, etc.; R9 = H, alkyl, etc.] and analogs useful for treating hyperproliferative disorders, were prepared E.g., a multi-step synthesis of I [X1 = N; R1 = indol-5-yl; R2 = H; R11 = Br], was given. Compounds I are effective at 0.2-2.5 g/day for a 70 kg human. 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 anticancer agent thienopyrimidine thienopyridine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products 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 May 28, 2009, Gottschling, Dirk; Dahmann, Georg; Doods, Henri; Heimann, Annekatrin; Mueller, Stephan Georg; Rudolf, Klaus; Schaenzle, Gerhard; Stenkamp, Dirk published a patent.Category: indole-building-block The title of the patent was Preparation of as 2-oxoindoles CGRP receptor antagonists. And the patent contained the following:

Title compounds I [R1 = 2-oxoindole with provisos; R2 = H, alkyl; R3 = H, alkylene, etc.; R4 = H, alkylene, etc.; U = N, N-oxide, CR5; V = N, N-oxide, CR6; X = N, N-oxide, CR7; Y = N, CR6; R5 = H, hyalo, CN, etc.; R6 = H, alkyl, etc.; R7 = H, halo, CN. etc.] and their pharmaceutically acceptable salts and formulations were prepared For example, coupling of chloropyrimide II and amine III afforded claimed oxoindole IV. In CGRP receptor antagonists assays, 4-examples of compounds I exhibited Ki values ranging from 15-535 nM. 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 oxoindole preparation cgrp receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines 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 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