Tag: 100-200

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

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 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 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 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 April 1, 1989, Muratake, Hideaki; Natsume, Mitsutaka published an article.Synthetic Route of 57817-04-6 The title of the article was Preparation of alkyl-substituted indoles in the benzene portion. Part 2. And the article contained the following:

Tosylpyrroles I (R1 = H, Me; R2 = H, Me, prenyl; R3 = alkyl, Ph, vinyl, protected CH2CH2CHO, H; Ts = tosyl) were treated with H2SO4 to give indoles II (R4 = Ts), which were converted to II (R4 = H). I were prepared from 1-tosyl-2-pyrrolecarboxaldehyde and 2-[3-(1,3-dioxolan-2-yl)propionyl]-1-tosylpyrrole. The experimental process involved the reaction of 7-Isopropyl-1H-indole(cas: 57817-04-6).Synthetic Route of 57817-04-6

The Article related to indole alkyl, alkylindole, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Synthetic Route of 57817-04-6

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

On December 8, 2020, Shi, Zhuangzhi; Dong, Ben published a patent.Category: indole-building-block The title of the patent was Preparation method of indole compound for improving yield. And the patent contained the following:

A simple preparation method of indole compound capable of improving yield, and easy to synthesize without any addnl. reducing agent is provided. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Category: indole-building-block

The Article related to indole preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Category: indole-building-block

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