Month: October 2022

On July 21, 2005, Nilsson, Magnus; Zhou, Xiao-Xiong; Oden, Lourdes; Classon, Bjorn; Noren, Rolf; Grabowska, Urszula; Jackson, Philip; Fallon, Philip; Carr, Andrew; Liley, Mark; Tozer, Matt; Johnson, Tony; Diaz, Victor; Crespo, Laia; Kangasmetsa, Jussi; Bonnaud, Thierry published a patent.Recommanded Product: Ethyl 6-methoxy-3-methylbenzofuran-2-carboxylate The title of the patent was Preparation of N- oxohexahydrofuropyrrole amino acid amides as cathepsin K inhibitors.. And the patent contained the following:

Title compounds [I; 1 of R1, R2 = halo, the other = H, halo; R3 = (fluoro)alkyl; R4 = H; R3R4C = (substituted) spirocycloalkyl, heterocyclyl; R5 = H, Me; E = CO, SOm, NR5SOm, NR5CO, CO2; R6 = stable (substituted) mono- or bicyclic carbocyclyl, heterocyclyl; m = 0-2], were prepared Thus, title compound (II) (multistep preparation given) inhibited cathepsin K with Ki = 5.3 nM. The experimental process involved the reaction of Ethyl 6-methoxy-3-methylbenzofuran-2-carboxylate(cas: 53724-96-2).Recommanded Product: Ethyl 6-methoxy-3-methylbenzofuran-2-carboxylate

The Article related to oxohexahydrofuropyrrole amino acid amide preparation cathepsin k inhibitor, osteoporosis gingivitis periodontitis pagets disease treatment amino acid amide, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Recommanded Product: Ethyl 6-methoxy-3-methylbenzofuran-2-carboxylate

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On August 29, 2013, Reiser, Ulrich; Bader, Gerd; Spevak, Walter; Steffen, Andreas; Parkes, Alastair L. published a patent.Recommanded Product: 60770-67-4 The title of the patent was Preparation of 5-alkynylpyridines as SMAC mimetics. And the patent contained the following:

This invention relates to 5-alkynyl-pyridines I [R1 = H or alkyl; R2, R21 = H, (fluoro)alkyl; R3 = (un)substituted C6-10 aryl, 5-14 membered heteroaryl; R4 = H, (un)substituted C6-10 aryl, 5-14 membered heteroaryl, etc.; R5 = H, halo, alkyl, etc.; or R4 and R5 taken together form C6-10 aryl, 5-14 membered heteroaryl], to their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. Over two-hundred compounds I were prepared E.g., a multi-step synthesis of II, starting from 5,6-dibromopyridin-2-amine and ethynyl-tri(propan-2-yl)silane, was described. Exemplified compounds I were tested in XIAP BIR3 and cIAP1 BIR3 binding assays (data given). The experimental process involved the reaction of 5-Iodobenzofuran(cas: 60770-67-4).Recommanded Product: 60770-67-4

The Article related to alkynylpyridine preparation smac mimetic antitumor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Recommanded Product: 60770-67-4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On May 22, 2009, Hong, Hui; Xu, Xiang; Yu, Jiaxin; Singh, Rajinder; Darwish, Ihab S.; Thota, Sambaiah published a patent.Electric Literature of 53724-96-2 The title of the patent was Preparation of phenylpiperidinyloxypyridine derivatives for use as therapeutic agents in metabolic disorders. And the patent contained the following:

Title compounds I [B = substituted aryl or heteroaryl; E = CO, SO2, or bond; T = alkyl-OR10, alkyl-C(O)R10, alkyl-S(O)p, etc.; Y = (un)substituted amine; each R4 independently = halo, CN. NO2, alkyl, etc.; or two R4 on the same carbon optionally combine to form oxo; R10 = H, alkyl, haloalkyl, etc.; m = 0 to 4; n = 0 to 3; p = 0 to 2; provided that when B = Ph, then E is not CO], and their pharmaceutically acceptable salts, are prepared and disclosed as therapeutic agents in metabolic disorders. Thus, e.g., II was prepared by deprotection of tert-Bu 1-(pyridin-4-ylmethyl)piperidin-4-ylcarbamate followed by amidation with 6-chloropicolinic acid, and etherification with 1-(4-(trifluoromethyl)phenyl)piperidin-4-ol. Select I were evaluated for their ability to activate AMPK using enzyme-linked immunosorbent assays, e.g., II demonstrated an EC50 value of 0.1-0.5 μM. The experimental process involved the reaction of Ethyl 6-methoxy-3-methylbenzofuran-2-carboxylate(cas: 53724-96-2).Electric Literature of 53724-96-2

The Article related to pyridine phenylpiperidinyloxy derivative preparation metabolic disorder, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Electric Literature of 53724-96-2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On October 6, 2005, El-Gezawy, Hani; Rettig, Wolfgang; Danel, Andrzej; Jonusauskas, Gediminas published an article.HPLC of Formula: 53724-96-2 The title of the article was Probing the Photochemical Mechanism in Photoactive Yellow Protein. And the article contained the following:

Selectively bridged model compounds related to the chromophore in photoactive yellow protein have been synthesized where the single bond adjacent to the benzene ring (bond 1) and where both bond 1 and the adjacent double bond (bond 2) are bridged. They were compared to the nonbridged reference compound regarding their photophys. properties using steady-state and time-resolved fluorescence at various temperatures Quantum chem. calculations were addnl. performed and showed that several conformers are populated in the ground state. The neutral model compounds show that the nonradiative deactivation channel is linked to both single- and double-bond twisting. The relative importance of single-bond twisting is increased for the corresponding deprotonated hydroxy compounds with an enhanced donor character. The simultaneous photochem. activity of both single and double bonds explains the ease of photochem. isomerization in the confined environment of the natural PYP protein and also of the primary step in the vision process in rhodopsin. The experimental process involved the reaction of Ethyl 6-methoxy-3-methylbenzofuran-2-carboxylate(cas: 53724-96-2).HPLC of Formula: 53724-96-2

The Article related to photoactive yellow protein photochem photophys chromophore model bridged compound, General Biochemistry: Proteins and Their Constituents and other aspects.HPLC of Formula: 53724-96-2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On January 15, 2021, Kobayashi, Jun-ichi; Hirasawa, Hideaki; Fujimori, Yoshikazu; Nakanishi, Osamu; Kamada, Noboru; Ikeda, Tetsuya; Yamamoto, Akitoshi; Kanbe, Hiroki published an article.Recommanded Product: 1459793-02-2 The title of the article was Identification of N-acyl-N-indanyl-α-phenylglycinamides as selective TRPM8 antagonists designed to mitigate the risk of adverse effects. And the article contained the following:

Transient receptor potential melastatin 8 (TRPM8), a temperature-sensitive ion channel responsible for detecting cold, is an attractive mol. target for the treatment of pain and other disorders. We have previously discovered a selective TRPM8 antagonist, KPR-2579, which inhibited bladder afferent hyperactivity induced by acetic acid instillation into the bladder. However, addnl. studies have revealed potential adverse effects with KPR-2579, such as the formation of a reactive metabolite, CYP3A4 induction, and convulsions. In this report, we describe the optimization of α-phenylglycinamide derivatives to mitigate the risk of these adverse effects. The optimal compound 13x exhibited potent inhibition against icilin-induced wet-dog shakes and cold-induced frequent voiding in rats, with a wide safety margin against the potential side effects. The experimental process involved the reaction of (S)-2,3-Dihydrobenzofuran-3-amine hydrochloride(cas: 1459793-02-2).Recommanded Product: 1459793-02-2

The Article related to trpm8 antagonist adverse event, cyp3a4 induction, oab, phenylglycinamide, reactive metabolite, trpm8, trpm8 antagonist, Pharmacology: Drug Interactions and General Pharmacology and other aspects.Recommanded Product: 1459793-02-2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On August 13, 2019, Chen, Qingcai; Zhao, Jun; Zhao, Xiaowei; Chen, Xiangfeng; Zong, Zaiwei; Lu, Hui published a patent.Application of 60770-67-4 The title of the patent was Nitrogen-containing heterocyclic compound, preparation method and application. And the patent contained the following:

The invention disclosed a kind of nitrogen-containing heterocyclic compound,its preparation method and application as potassium ion competitive acid retardant or gastric acid secretion inhibitor. The claimed compound is shown in structure I (ring A = saturated or unsaturated five member ring; X1,X2,X3 = C, N, O, S, etc.; a,b = bridge atom C or N; R1 = -SO2R4, -(CH2)nR4, or -CHR4R5; R4 = aryl, arylalkyl, arylalkenyl, benzocyclo, etc.; R5 = halo, nitro, cyano, etc.; n = 0, 1-6 integers; R2 = aryl, arylalkyl, heteroaryl, etc.; R3 = H, alkyl cycloalkyl). The claimed compound is prepared via multiple steps (example procedure given). The prepared compound has proton pump H+/K+-ATP enzyme inhibition effect, and is used for preventing and treating diseases related to inhibition of gastric acid secretion, such as peptic ulcer, zollinger-ellison syndrome, gastritis, erosive esophagitis, reflux esophagitis, symptomatic gastroesophageal reflux disease and the like. The experimental process involved the reaction of 5-Iodobenzofuran(cas: 60770-67-4).Application of 60770-67-4

The Article related to nitrogen containing heterocycle preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Application of 60770-67-4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On August 15, 2019, Chen, Qingcai; Zhao, Jun; Zhao, Xiaowei; Chen, Xiangfeng; Zong, Zaiwei; Lu, Hui published a patent.Application of 60770-67-4 The title of the patent was Nitrogen-containing heterocyclic compound, preparation method and application. And the patent contained the following:

The invention disclosed a kind of nitrogen-containing heterocyclic compound,its preparation method and application as potassium ion competitive acid retardant or gastric acid secretion inhibitor. The claimed compound is shown in structure I (ring A = saturated or unsaturated five member ring; X1,X2,X3 = C, N, O, S, etc.; a,b = bridge atom C or N; R1 = -SO2R4, -(CH2)nR4, or -CHR4R5; R4 = aryl, arylalkyl, arylalkenyl, benzocyclo, etc.; R5 = halo, nitro, cyano, etc.; n = 0, 1-6 integers; R2 = aryl, arylalkyl, heteroaryl, etc.; R3 = H, alkyl cycloalkyl). The claimed compound is prepared via multiple steps (example procedure given). The prepared compound has proton pump H+/K+-ATP enzyme inhibition effect, and is used for preventing and treating diseases related to inhibition of gastric acid secretion, such as peptic ulcer, zollinger-ellison syndrome, gastritis, erosive esophagitis, reflux esophagitis, symptomatic gastroesophageal reflux disease and the like. The experimental process involved the reaction of 5-Iodobenzofuran(cas: 60770-67-4).Application of 60770-67-4

The Article related to nitrogen containing heterocycle preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Application of 60770-67-4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On September 25, 2008, Cai, Xiong; Qian, Changgeng; Zhai, Haixiao published a patent.Computed Properties of 60770-67-4 The title of the patent was Preparation of imidazo[4,5-c]pyridine derivatives as HSP90 inhibitors. And the patent contained the following:

Title compounds represented by the formula I [wherein U = N or CH; W = H, halo, amino, etc.; X = absent, O, S, etc.; Y = independently H, halo, NO2, CN or alkyl; Z = (alkylcarbonyl)amino or (di)alkylamino; Q = (un)substituted (hetero)aryl or (Hetero)cycloalkyl; V = H, (un)substituted aryl, alkenyl, etc.; and geometric isomers, enantiomers, diastereomers, racemates, pharmaceutically acceptable salts, prodrugs and solvates thereof] were prepared as HSP90 inhibitors. For example, II was provided in a multi-step synthesis starting from N-(4-pentynyl)phthalimide. I were tested for inhibiting HSP90 chaperone activity in vitro assay and HSP90 competition binding (Fluorescence Polarization) assay. Thus, I and their pharmaceutical compositions are useful as HSP90 inhibitors for the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease. The experimental process involved the reaction of 5-Iodobenzofuran(cas: 60770-67-4).Computed Properties of 60770-67-4

The Article related to imidazopyridine preparation hsp90 inhibitor cancer autoimmune neurodegenerative disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Computed Properties of 60770-67-4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On August 18, 2011, Marom, Ehud; Mizhiritskii, Michael; Rubnov, Shai published a patent.Related Products of 60770-67-4 The title of the patent was Process for preparation of Dronedarone and synthetic intermediates thereof. And the patent contained the following:

The present invention provides several synthetic methods for preparing N-(2-butylbenzofuran-5-yl)-N-(methylsulfonyl)methanesulfonamide, an intermediate in the preparation of Dronedarone. For example, a mixture of CuI, bis(methanesulfonyl)amine, N,N-dimethylglycine, K3PO4, 5-bromo-2-butylbenzofuran (preparation given), and DMF was refluxed for 24-48 h to afford N-(2-butylbenzofuran-5-yl)-N-(methylsulfonyl)methanesulfonamide. The intermediate obtained above was reacted with 4-[3-(dibutylamino)propoxy]benzoyl chloride hydrochloride in the presence of aluminum chloride in dry dichloromethane at 5 – 10 °C overnight to afford N-[2-butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]benzofuran-5-yl]-N-methylsulfonylmethanesulfonamide, which was treated with 5 M NaOH in THF at room temperature for 3 h to give Dronedarone as the final product. The experimental process involved the reaction of 5-Iodobenzofuran(cas: 60770-67-4).Related Products of 60770-67-4

The Article related to preparation dronedarone benzofuran, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenofurans and other aspects.Related Products of 60770-67-4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On February 21, 2013, Marom, Ehud; Mizhiritskii, Michael; Rubnov, Shai published a patent.Product Details of 60770-67-4 The title of the patent was Preparation of benzofurans and use thereof as synthetic intermediates. And the patent contained the following:

The present invention provides several synthetic methods for preparing N-(2-butylbenzofuran-5-yl)-N-(methylsulfonyl)methanesulfonamide, a compound of formula (3), an intermediate in the preparation of Dronedarone. The present invention further provides a process for preparing Dronedarone, comprising the steps of converting 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) to Dronedarone, wherein the 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) is prepared by the processes of the present invention. The experimental process involved the reaction of 5-Iodobenzofuran(cas: 60770-67-4).Product Details of 60770-67-4

The Article related to preparation dronedarone benzofuran, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenofurans and other aspects.Product Details of 60770-67-4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem