Month: November 2022

On March 17, 2016, Nagamochi, Masatoshi; Gotanda, Kentoku; Noguchi, Tetsuji; Goto, Taiji; Sasaki, Junko; Torihata, Munefumi; Yoshino, Toshiharu; Isobe, Takashi; Ramadass, Venkataramanan published a patent.Recommanded Product: 4-Bromo-5-methoxy-2-methylaniline The title of the patent was Preparation of carboxylic acid derivatives as RORγt (retinoic acid receptor-related orphan receptor γt) inhibitors. And the patent contained the following:

Title compounds I [R1 = alkyl, cycloalkyl or phenyl; R2 = H, halo, alkyl, etc.; R3 = H, carboxy-alkyl or hydroxy; R4 = halo or alkyl; R5 = H or alkyl; R6 = H, halo or alkyl; R7 = H, halo, alkyl, etc.; R8 = hydroxy, alkoxy, monoalkylamino, etc.; L = single bond, methylene or oxygen atom; E = phenylene (optionally substituted with halo, alkyl or alkylsulfonyl), pyridinylene (optionally substituted with halo, alkyl or alkylsulfonyl), thienylene, etc.; Q1 = nitrogen atom or CH; Q2 = nitrogen atom or CH; -U-T- = -CH2CH2- or -CH:CH-; Y = methylene or oxygen atom; V = nitrogen atom or C(R9); R9 = H, alkyl, cycloalkyl, etc.; or pharmaceutically acceptable salts thereof], useful for the treatment of psoriasis, psoriatic arthritis, etc., were prepared For example, EDCI-mediated amidation of II [R = OH] (prepared from 1-bromo-4-iodo-2-methylbenzene in a multi-step process) with methylamine·HCl afforded compound II [R = NHMe]. In IL-17 production inhibition assay, 81-example of I showed IC50 values (nM) ranging from 4.48 to 1110, e.g., IC50 of II [R = NHMe] was 4.48 nM. Pharmaceutical compositions comprising I are disclosed. The experimental process involved the reaction of 4-Bromo-5-methoxy-2-methylaniline(cas: 152626-77-2).Recommanded Product: 4-Bromo-5-methoxy-2-methylaniline

The Article related to carboxylic acid preparation ror gamma t inhibitor, psoriasis psoriatic arthritis treatment ror gamma t inhibition, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 4-Bromo-5-methoxy-2-methylaniline

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Yao, Lingyun; Shang, Yan; Wang, Jian-Shu; Pan, Ailin; Ying, Jun; Wu, Xiao-Feng published an article in 2021, the title of the article was Palladium-catalyzed carbonylative cyclization of 2-alkynylanilines and aryl iodides to access N-acyl indoles.Quality Control of 2-((4-Methoxyphenyl)ethynyl)aniline And the article contains the following content:

A palladium-catalyzed carbonylative synthesis of N-acyl indoles I (R = Ph, 2-methylphenyl, 4-chloropenyl, 3,4-dimethylphenyl, etc.; R1 = Ph, 3-methylphenyl, 4-methylphenyl, 4-methoxyphenyl, 4-fluorophenyl; R2 = H, F) from 2-alkynylanilines 2-NH25-R2C6H3CCR1 and aryl iodides RI has been developed. Using benzene-1,3,5-triyl triformate (TFBen) as the CO source, the reaction produced a variety of N-acyl indoles I in a facile manner with high yields. The experimental process involved the reaction of 2-((4-Methoxyphenyl)ethynyl)aniline(cas: 157869-15-3).Quality Control of 2-((4-Methoxyphenyl)ethynyl)aniline

The Article related to acyl indole preparation, alkynylaniline aryl iodide benzenetriyl triformate carbonylative cyclization palladium catalyst, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Quality Control of 2-((4-Methoxyphenyl)ethynyl)aniline

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

On February 9, 1995, Achard, Daniel; Grisoni, Serge; James-Surcouf, Evelyne; Malleron, Jean-Iuc; Morgat, Anne; Peyronel, Jean-Francois; Sabuco, Jean-Francois; Tabart, Michel published a patent.Related Products of 81616-80-0 The title of the patent was Preparation of N-acyl-4-hydroxyperhydroisoindoles as substance P antagonists. And the patent contained the following:

Title compounds [I; 1 of R = H, OH, (hydroxy)alkyl and the other = H, (hydroxy)alkyl, Ph; R1 = Ph, alkyl, alkoxy, etc.; R2 = H, halo, OH, alkyl,alkoxy, etc.; R3 = (un)substituted Ph; R4 = OH; R4 = F when R5,R15 = H or alkyl; 1 of R5,R15 = H, OH, alkyl and the other = H or alkyl; R4R5 = bond; R6 = H, OH, (hydroxy)alkyl] were prepared Thus, 5-methylcyclohex-2-en-1-one was cyclocondensed with PhCH2N(CH2OBu)CH2SiMe3 and the product condensed with BuLi-treated PhOMe to give, after deprotection and N-acylation by (S)-2-(MeO)C6H4CHMeCO2H, title compound (3aR*,4R*,6S*,7aS*)-II which had ED50 of 0.07mg/kg i.v. for inhibition of substance P-induced capillary permeability in monkeys. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Related Products of 81616-80-0

The Article related to acylhydroxyperhydroisoindole preparation substance p antagonist, isoindole acylhydroxyperhydro preparation substance p antagonist, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Related Products of 81616-80-0

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

On April 21, 2022, Ito, Mamoru; Onoda, Hideaki; Takaki, Asahi; Shibata, Takanori published an article.COA of Formula: C15H13NO The title of the article was Gold-Catalyzed Cascade and Divergent Synthesis of Indolobenzazepines and Indoloquinolines from Nitrogen-Tethered 1,8-Diynes. And the article contained the following:

Authors describe the divergent construction of two nitrogen-containing polycyclic systems by gold-catalyzed cycloisomerizations. The gold-catalyzed cascade hydroamination and 7-endo-dig-selective cycloisomerization of nitrogen-tethered 1,8-diynes yielded indolo[1,7-ab]benzazepines in one pot. In contrast, when Johnphos-coordinated gold catalyst was used, the same 1,8-diynes were transformed into indolo[1,2-a]quinolines by 6-endo-dig-selective cycloisomerization along with rearrangement of the substituent on one of the alkynes. The reaction of a naphthalene-tethered substrate provided a helically chiral aza[6]helicene. The experimental process involved the reaction of 2-((4-Methoxyphenyl)ethynyl)aniline(cas: 157869-15-3).COA of Formula: C15H13NO

The Article related to indolobenzazepine indoloquinoline preparation, nitrogen tethered diyne tandem hydroamination cycloisomerization rearrangement gold, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C15H13NO

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Xu, Fan; Smith, Myles W. published an article in 2021, the title of the article was A general approach to 2,2-disubstituted indoxyls: total synthesis of brevianamide A and trigonoliimine C.Related Products of 578-58-5 And the article contains the following content:

The indoxyl unit is a common structural motif in alkaloid natural products and bioactive compounds Herein, a general method that transforms readily available 2-substituted indoles into 2,2-disubstituted indoxyls via nucleophile coupling with a 2-alkoxyindoxyl intermediate and showcase its utility in short total syntheses of the alkaloids brevianamide A (7 steps) and trigonoliimine C (6 steps) is reported. The developed method is operationally simple and demonstrates broad scope in terms of nucleophile identity and indole substitution, tolerating 2-alkyl substituents and free indole N-H groups, elements beyond the scope of most prior approaches. Spirocyclic indoxyl products are also accessible via intramol. nucleophilic trapping. The experimental process involved the reaction of 2-Methylanisole(cas: 578-58-5).Related Products of 578-58-5

The Article related to indoxyl preparation, indole nucleophile coupling, brevianamide a trigonoliimine c total synthesis, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Related Products of 578-58-5

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

On February 14, 2018, Chaisan, Nattawadee; Kaewsri, Wilailak; Thongsornkleeb, Charnsak; Tummatorn, Jumreang; Ruchirawat, Somsak published an article.Category: ethers-buliding-blocks The title of the article was PtCl4-catalyzed cyclization of N-acetyl-2-alkynylanilines: A mild and efficient synthesis of N-acetyl-2-substituted indoles. And the article contained the following:

An efficient synthesis of N-acetyl-2-substituted indole derivatives via direct intramol. hydroamination of N-acetyl-2-alkynylaniline derivatives was developed. The reaction could be applied to a wide range of substrates employing only 1-2 mol% of PtCl4 as the catalyst to furnish the desired indole products in moderate to excellent yields. The current protocol is efficient, reliable and scalable, and could serve as an important tool for convenient and rapid access to this important class of N-heterocyclic skeleton from readily available substrates. The experimental process involved the reaction of 2-((4-Methoxyphenyl)ethynyl)aniline(cas: 157869-15-3).Category: ethers-buliding-blocks

The Article related to indole acetyl substituted preparation acetylalkynylaniline cyclization platinum chloride catalyst, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Category: ethers-buliding-blocks

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

On February 7, 2020, Yuan, Shuo; Zhang, Dan-Qing; Zhang, Jing-Ya; Yu, Bin; Liu, Hong-Min published an article.HPLC of Formula: 157869-15-3 The title of the article was Palladium-Catalyzed Ligand-Free Double Cyclization Reactions for the Synthesis of 3-(1′-Indolyl)-phthalides. And the article contained the following:

Indole and phthalide are privileged heterocyclic scaffolds in numerous natural products and bioactive mols. The synthesis and biol. evaluation of the compounds combining these two scaffolds have rarely been reported. The first palladium-catalyzed ligand-free double cyclization reactions that enable efficient synthesis of 3-(1′-indolyl)-phthalides, e.g., I, under mild conditions is reported. Notably, only 1.0 mol % of catalyst loading is used, suggesting high efficiency. Late-stage elaborations give highly functionalized analogs. The experimental process involved the reaction of 2-((4-Methoxyphenyl)ethynyl)aniline(cas: 157869-15-3).HPLC of Formula: 157869-15-3

The Article related to ethynylaniline formylbenzoic acid palladium catalyst cascade cyclization, indolyl phthalide preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.HPLC of Formula: 157869-15-3

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

On March 3, 2017, Li, Yi-Jin; Yan, Na; Liu, Chun-Hua; Yu, Yang; Zhao, Yu-Long published an article.Application In Synthesis of 2-((4-Methoxyphenyl)ethynyl)aniline The title of the article was Gold/Copper-Co-catalyzed Tandem Reactions of 2-Alkynylanilines: A Synthetic Strategy for the C2-Quaternary Indolin-3-ones. And the article contained the following:

A new strategy for direct and highly efficient synthesis of 2,3′-bisindolin-3-ones has been developed via a gold/copper-co-catalyzed tandem reactions of 2-alkynylanilines using TBHP as the terminal oxidant and oxygen-atom source. The single-step process involves a novel tandem intermol. nucleophilic addition, intramol. cyclization/oxidative cross-dehydrogenative coupling where up to four new bonds and two indole rings were created simultaneously in one-pot manner. The reaction features a broad substrate scope, good functional group tolerance, and high atom-economy. The experimental process involved the reaction of 2-((4-Methoxyphenyl)ethynyl)aniline(cas: 157869-15-3).Application In Synthesis of 2-((4-Methoxyphenyl)ethynyl)aniline

The Article related to bisindolinone preparation, gold copper cocatalyst alkynylaniline, aniline alkynyl gold copper cocatalyst, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Application In Synthesis of 2-((4-Methoxyphenyl)ethynyl)aniline

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

On October 28, 1993, Achard, Daniel; Grisoni, Serge; Malleron, Jean Luc; Peyronel, Jean-francois; Tabart, Michel published a patent.Application In Synthesis of (S)-2-(2-Methoxyphenyl)propanoic acid The title of the patent was Perhydroisoindole derivatives as substance P antagonists and their preparation. And the patent contained the following:

Title compounds I [R = Ph optionally substituted with halogen or Me in position 2 or 3; R1 = (un)substituted Ph, cyclohexadienyl, naphthyl, indenyl, heterocyclyl; R2 = H, halo, OH, alkyl, aminoalkyl, CO2H, amino, etc.; R3 = Ph optionally substituted in position 2 by C1-2 alkyl or alkoxy; R4 = F, OH; R5 = H; or R4 = R5 = OH; or R4R5 = bond] and their stereoisomers, isomer mixtures, and salts, are claimed (40 synthetic examples). For example, N-acylation of [3a(S),4(S),7a(S)]-7,7-diphenyl-4-(2-methoxyphenyl)perhydroisoindol-4-ol (prepared in 4 steps) with (S)-2-(MeO)C6H4CHMeCO2H (prepared in 3 steps) using EDCI in CH2Cl2 gave title compound II. The ED50 of II for inhibition of increased capillary permeability induced by septide (a substance P agonist) in guinea pigs was 0.04 mg/kg i.v. or 3.5 mg/kg p.o. II also countered hypotension and bronchoconstriction induced by substance P in guinea pigs. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Application In Synthesis of (S)-2-(2-Methoxyphenyl)propanoic acid

The Article related to perhydroisoindole preparation substance p antagonist, isoindole perhydro preparation substance p antagonist, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Application In Synthesis of (S)-2-(2-Methoxyphenyl)propanoic acid

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

On October 28, 2015, Li, Yin-Long; Li, Jian; Yu, Sheng-Nan; Wang, Ji-Bo; Yu, Yan-Min; Deng, Jun published an article.Quality Control of 2-((4-Methoxyphenyl)ethynyl)aniline The title of the article was A concise approach for the synthesis of 3-iodoindoles and 3-iodobenzo[b]furans via Ph3P-catalyzed iodocyclization. And the article contained the following:

A variety of 3-iodoindole and 3-iodobenzo[b]furan derivatives were conveniently prepared from the corresponding 2-alkynylanilines and 2-alkynylphenols through Ph3P-catalyzed iodocyclization in the presence of N-iodosuccinimide. This protocol provides a rapid access to 3-iodoindoles and 3-iodobenzo[b]furans in good to excellent yields under mild conditions. The experimental process involved the reaction of 2-((4-Methoxyphenyl)ethynyl)aniline(cas: 157869-15-3).Quality Control of 2-((4-Methoxyphenyl)ethynyl)aniline

The Article related to iodoindole iodobenzofuran preparation, iodocyclization alkynylphenol alkynylaniline triphenylphosphine catalyst, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Quality Control of 2-((4-Methoxyphenyl)ethynyl)aniline

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem