Day: November 4, 2022

On August 20, 2020, Lee, Matthew Randolph; Varano Jr., Anthony Joseph; Bobinski, Thomas P. published a patent.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Sulfonylisoquinolinone derivatives as ROCK kinase inhibitors and their preparation. And the patent contained the following:

The present invention relates to compounds that inhibit ROCK activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of inhibiting ROCK activity and methods for treating, for example cerebral cavernous malformation syndrome (CCM) and cardiovascular diseases using the compounds and pharmaceutical compositions of the present invention. Example compound I 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 I. The invention compounds were evaluated for their ROCK kinase inhibitory activity. From the assay, it was determined that compound I exhibited IC50 value in the range of 1,000 nM to ≤ 10,000 nM. 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 sulfonylisoquinolinone preparation rock kinase inhibitor, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines 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 September 11, 2013, Wang, Chao; Jiang, Xue; Wei, Yawen; Xue, Dong; Xiao, Jianliang published a patent.Recommanded Product: 52537-00-5 The title of the patent was N-Methylation method of aromatic amine. And the patent contained the following:

The invention relates to the N-methylation method of aromatic amines. N-Methylarom. amines were prepared via N-methylation of arylamines with formic acid. The invention has simple operation and wide application range of substrate, and can obtain high-yield N-methylated aromatic amine without catalytic condition. 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 arylamine formic acid methylation, methyl arylamine preparation, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines 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

Zhang, Jingyu; Chen, Shiya; Chen, Fangfang; Xu, Wensheng; Deng, Guo-Jun; Gong, Hang published an article in 2017, the title of the article was Dehydrogenation of Nitrogen Heterocycles Using Graphene Oxide as a Versatile Metal-Free Catalyst under Air.Related Products of 52537-00-5 And the article contains the following content:

Graphene oxide (GO) has been developed as an inexpensive, environmental friendly, metal-free carbocatalyst for the dehydrogenation of nitrogen heterocycles. Valuable compounds, such as quinoline, 3,4-dihydroisoquinoline, quinazoline, and indole derivatives, have been successfully used as substrates. The investigation of various oxygen-containing mols. with different conjugated systems indicated that both the oxygen-containing groups and large π-conjugated system in GO sheets are essential for this reaction. 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 graphene oxide nitrogen heterocycle dehydrogenation catalyst green chem, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines 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 February 18, 2014, Kasperkiewicz, Paulina; Poreba, Marcin; Snipas, Scott J.; Parker, Heather; Winterbourn, Christine C.; Salvesen, Guy S.; Drag, Marcin published an article.Product Details of 79815-20-6 The title of the article was Design of ultrasensitive probes for human neutrophil elastase through hybrid combinatorial substrate library profiling. And the article contained the following:

The exploration of protease substrate specificity is generally restricted to naturally occurring amino acids, limiting the degree of conformational space that can be surveyed. We substantially enhanced this by incorporating 102 unnatural amino acids to explore the S1-S4 pockets of human neutrophil elastase (NE). This approach provides hybrid natural and unnatural amino acid sequences, and thus we termed it the Hybrid Combinatorial Substrate Library (HyCoSuL). Library results were validated by the synthesis of individual tetrapeptide substrates, with the optimal substrate demonstrating more than three orders of magnitude higher catalytic efficiency than commonly used substrates of elastase. This optimal substrate was converted to an activity-based probe that demonstrated high selectivity and revealed the specific presence of active elastase during the process of neutrophil extracellular trap formation. We propose that this approach can be successfully used for any type of endopeptidase to deliver high activity and selectivity in substrates and probes. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Product Details of 79815-20-6

The Article related to peptide library optimal substrate neutrophil elastase activity based probe, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.Product Details 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 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 August 16, 2019, Sen, Chiranjit; Sahoo, Tapan; Singh, Harshvardhan; Suresh, Eringathodi; Ghosh, Subhash Chandra published an article.Application In Synthesis of Methyl 2-methyl-1H-indole-3-carboxylate The title of the article was Visible Light-Promoted Photocatalytic C-5 Carboxylation of 8-Aminoquinoline Amides and Sulfonamides via a Single Electron Transfer Pathway. And the article contained the following:

An efficient photocatalytic method was developed for the remote C5-H bond carboxylation of 8-aminoquinoline amide and sulfonamide derivatives This methodol. uses in situ generated •CBr3 radical as a carboxylation agent with alc. and is further extended to a variety of arenes and heteroarenes to synthesize the desired carboxylated product in moderate-to-good yields. The reaction proceeding through a single electron transfer pathway was established by a control experiment, and a butylated hydroxytoluene-trapped aryl radical cation intermediate in high-resolution mass spectrometry was identified. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Application In Synthesis of Methyl 2-methyl-1H-indole-3-carboxylate

The Article related to aminoquinoline amide sulfonamide carboxylation photocatalyst electron transfer pathway, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application In Synthesis of Methyl 2-methyl-1H-indole-3-carboxylate

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 31, 1977, Kitamura, Reiko; Fujii, Harue; Hashiba, Kazuhiko; Somei, Masanori; Kaneko, Chikara published an article.Related Products of 65417-22-3 The title of the article was Studies on the N-oxides of π-deficient N-heteroaromatics. Part XXVII. Ring-contraction reactions of methyl benz[d]-3,1-oxazepine 5-carboxylates. And the article contained the following:

Irradiation of the quinoline oxide I (R = Ph, R1 = H) in Me2CO for 5 h gave 82% Me 2-phenylindole-3-carboxylate (II; R = Ph) and 9% Me 2-phenylquinoline-4-carboxylate. If the irradiation was terminated after 20 mins, ∼80% oxazepine III (R = Ph, R1 = H) was obtained, which on further irradiation, or on refluxing in MeOH in the dark (10 h) gave II (R = Ph). Similar irradiation of I (R = Me, R1 = H) in Me2CO or MeCN gave the phenylindole II (R = Me). Irradiation of I (R = Ph, R1 = Me) gave the oxazepine III (R = Ph, R1 = Me) which on heating in MeOH in a sealed tube for 2 h at 100° gave 21% II (R = Ph) and 23% 3H-indole IV (R = Ph, R1 = Me), the latter being converted into II (R = Ph) by heating in MeOH (100° in a sealed tube, 4 h) or in MeOH at room temperature in presence of HCl or KOH. Therefore the Me quinolinecarboxylates I were converted into the Me indolecarboxylates II via the oxazepines III and the 3H-indoles IV. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Related Products of 65417-22-3

The Article related to quinolinecarboxylate oxide photolysis, benzoxazepinecarboxylate ring contraction, indolecarboxylate, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Related Products of 65417-22-3

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

Banini, Serge R.; Turner, Michael R.; Cummings, Matthew M.; Soederberg, Bjoern C. G. published an article in 2011, the title of the article was A base-modulated chemoselective synthesis of 3-cyanoindoles or 4-cyanoquinolines using a palladium-catalyzed N-heterocyclization.Electric Literature of 65417-22-3 And the article contains the following content:

A selective methodol. for the synthesis of either 3-cyanoindoles or 4-cyanoquinolines via a base-modulated palladium-catalyzed reductive N-heterocyclization from a common 1-cyano-1-(2-nitrophenyl)-1-alkene precursor is described. The required starting materials were prepared either by a Kosugi-Migita-Stille coupling of 2-halo-1-nitrobenzenes with a tributyl(1-alkenyl)stannane or by a vicarious nucleophilic substitution of nitrobenzenes followed by a Knoevenagel condensation with an aldehyde. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Electric Literature of 65417-22-3

The Article related to nitrophenylalkenenitrile chemoselective cyclization indolecarbonitrile quinolinecarbonitrile preparation, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Electric Literature of 65417-22-3

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 November 26, 1990, Torii, Sigeru; Okumoto, Hiroshi; Xu, Long He published an article.Product Details of 65417-22-3 The title of the article was A direct approach to 2-substituted 1,4-dihydro-4-oxoquinoline-3-carboxylates by palladium-catalyzed carbonylative cyclization. And the article contained the following:

Carbonylation of 3-substituted 3-(2-haloarylamino)prop-2-enoates I (R = Me, CH2CO2Me, CO2Me, R1 = R2 = H, R3 = Br, iodo; R = Me, R1 = R2 = F, R3 = Br; R = Me, CH2CO2Me, R1 = F, R2 = Cl, R3 = Br) in the presence of Pd(OAc)2 under 20 kgcm-2 of CO at 120° resulted in heterocyclization to form a variety of 2-substituted 1,4-dihydro-4-oxoquinoline-3-carboxylates II in good yields. Lactones III (R1 = R2 = H; R1 = F, R2 = Cl) were prepared similarly. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Product Details of 65417-22-3

The Article related to cyclocarbonylation haloarylaminopropenoate palladium catalyst, quinolinecarboxylate dihydro oxo, propenoate haloarylamino cyclocarbonylation palladium catalyst, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Product Details of 65417-22-3

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