Tag: 100-200

On February 3, 2005, Cheng, Jie Fei; Nguyen, Bao Ngoc; Liu, Xuewei; Lopaschuk, Gary D.; Dyck, Jason R. published a patent.Product Details of 29735-85-1 The title of the patent was Preparation of heterocyclic compounds useful as malonyl-CoA decarboxylase inhibitors. And the patent contained the following:

The present invention provides methods for the use of compounds I [X1, X2, X3 = O, N, NH, NR5, S, C; R1, R2 = H, halogen, substituted C1-6-alkyl, substituted C1-6-alkenyl, substituted C1-6-alkynyl, alkoxy, (un)substituted Ph, aryl, (un)substituted heteroaryl, NHCONR5R6, COR5, CONR5R6, S(O)nR5, SO2NR5R6; R3, R4 = H, Br, Cl, F, I, OH, OMe, CO2H, CO2R5, CONR5R6, S(O)nR5, SO2NR5R6, substituted C1-6-alkyl, C1-6-alkoxy, (un)substituted Ph, aryl, heteroaryl; R5, R6 = H, (un)substituted C1-6-alkyl, (un)substituted Ph, aryl, heteroaryl], its enantiomers, diastereomers, tautomers, or physiol. acceptable salts or prodrugs, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. Thus, benzofuran I [X1 = CC(:O)NHC6H3(OMe)2-3,4, X2 = CH, X3 = O, R3 = 4-Br, R4 = 6-Br] was prepared from 5-methoxybenzofuran-2-carboxylic acid via regioselective bromination at C(3), decarboxylation, debromination-carboxylation at C(3), O-demethylation, regioselective dibromination and amidation with 3,4-dimethoxyaniline. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. The inhibitory activity of I vs. malonyl-CoA decarboxylase was determined [Ki = 31.6 – 4750.2 μM]. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity. The experimental process involved the reaction of 5-Hydroxybenzofuran-3-carboxylic acid(cas: 29735-85-1).Product Details of 29735-85-1

The Article related to heterocyclic compound preparation malonyl coa decarboxylase inhibitor, cardiovascular disease prophylaxis management treatment heterocyclic compound, diabetes prophylaxis management treatment heterocyclic compound, cancer prophylaxis management treatment heterocyclic compound, obesity prophylaxis management treatment heterocyclic compound and other aspects.Product Details of 29735-85-1

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

On November 13, 2014, Hirasawa, Hideaki; Kawamura, Naohiro; Kobayashi, Junichi published a patent.Product Details of 1459793-02-2 The title of the patent was Preparation of α-substituted glycine amides as TRPM8 inhibitors. And the patent contained the following:

Title compounds I [A1 = C6-10 aryl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.), 5-membered heterocyclyl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.) or 6-membered heterocyclyl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.); A2 = C6-10 aryl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.), heterocyclyl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.) or C3-6 cycloalkyl; X = CH or N; Y = -CR1R2- or oxygen atom; R1, R2 = independently H, halo or C1-6 alkyl; R3, R4 = independently H, halo, C1-6 alkyl, etc.; n = 1 or 2; or pharmacol. acceptable salts thereof] were prepared For example, to a solution of (R)-4,6-difluoroindan-1-ylamine (0.1 g) in methanol (1 mL) was added benzaldehyde (0.063 g), the resulting mixture was stirred at 60° for 1 h, treated with nicotinic acid (0.073 g) and 4-phenylcyclohexen-1-ylisocyanide (0.108 g) [room temperature → 60° (overnight)], cooled to room temperature, concentrated in vacuo, and treated with THF (3 mL), water (12 μL) and HCl (4 mol/L in dioxane, 440 μL) at room temperature for 1.5 h to give, after work-up, compound II (0.076 g). The invention compounds showed potent inhibitory effect on icilin-induced wet-dog shaking in rat. Compounds I are claimed useful for the treatment of diseases or conditions associated with afferent nerve hyperexcitability or injury. The experimental process involved the reaction of (S)-2,3-Dihydrobenzofuran-3-amine hydrochloride(cas: 1459793-02-2).Product Details of 1459793-02-2

The Article related to glycine amide preparation trpm8 inhibitor, nerve hyperexcitability disease treatment glycine amide trpm8 inhibition, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Benzocyclopropenes, Benzocyclobutenes, and Indenes and other aspects.Product Details of 1459793-02-2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Lena, Gersande; Trapani, Joseph A.; Sutton, Vivien R.; Ciccone, Annette; Browne, Kylie A.; Smyth, Mark J.; Denny, William A.; Spicer, Julie A. published their research in Journal of Medicinal Chemistry on December 11 ,2008. The article was titled 《Dihydrofuro[3,4-c]pyridinones as Inhibitors of the Cytolytic Effects of the Pore-Forming Glycoprotein Perforin》.SDS of cas: 53860-74-5 The article contains the following contents:

Dihydrofuro[3,4-c]pyridinones are the first class of small mols. reported to inhibit the cytolytic effects of the lymphocyte toxin perforin. A lead structure was identified from a high throughput screen, and a series of analogs I (X = O, S; Y = O, NH; R = Ph, 4-FC6H4, 2-furyl, 5-methyl-2-thienyl, 3-thienyl, 2-benzofuryl, 3-benzothienyl, 3-indolyl, etc.) were designed and prepared to explore structure-activity relationships around the core bicyclic ring and pendant aryl(heteroaryl) ring. This resulted in the identification of a submicromolar inhibitor of the perforin-induced lysis of Jurkat T-lymphoma cells. After reading the article, we found that the author used 6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5SDS of cas: 53860-74-5)

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.SDS of cas: 53860-74-5Benzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Hirota, Takashi; Fujita, Hiroko; Sasaki, Kenji; Namba, Tetsuto published their research in Journal of Heterocyclic Chemistry on December 31 ,1986. The article was titled 《A novel synthesis of benzofuran and related compounds. III. The Vilsmeier reaction of phenoxyacetaldehyde diethyl acetals》.Application of 53860-74-5 The article contains the following contents:

2-Benzofurancarboxaldehydes, e.g., I (R = H, OMe; R1 = OMe, OEt, NEt2) were prepared in 15-58% yields by the Vilsmeier reaction 3,5-RR1C6H3OCH2CH(OEt)2 (II). A rare geminidiol III was isolated in one case. II were prepared in 65-91% yields by treating 3,5-RR1C6H3ONa with BrCH2CH(OEt)2. In the experiment, the researchers used 6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5Application of 53860-74-5)

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.Application of 53860-74-5Benzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

In 1977,European Journal of Medicinal Chemistry included an article by Fatome, Marc; Andrieu, Louis; Laval, Jean Denis; Clavel, Jean Marc; Blanco, Luis; Guillaumel, Jean; Rene, Loic; Royer, Rene. Safety of 6-Methoxybenzofuran-2-carbaldehyde. The article was titled 《Comparison of radioprotective activities of similar substituted derivatives of benzofurane and 2H-chromene》. The information in the text is summarized as follows:

The radioprotective activities of I(R1, R2, R3, R4 = H, OMe; Z = MeCO, CHO, CN, CO2Et) were less than those of II (same substituents as I). In the experiment, the researchers used many compounds, for example, 6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5Safety of 6-Methoxybenzofuran-2-carbaldehyde)

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.Safety of 6-Methoxybenzofuran-2-carbaldehydeBenzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

《Synthesis and some CNS activities of new benzofuranylacryloylpiperazines》 was published in European Journal of Medicinal Chemistry in 1995. These research results belong to Dauzonne, D.; Gillardin, J. M.; Lepage, F.; Pointet, R.; Risse, S.; Lamotte, G.; Demerseman, P.. Quality Control of 6-Methoxybenzofuran-2-carbaldehyde The article mentions the following:

A series of novel [(benzofuranyl)acryloyl]piperazines, which are structurally related to both cinnamide derivatives and befuraline, have been prepared as their hydrochlorides. Their anticonvulsant and antidepressant activities against seizures induced by electroshock and against tetrabenazine-induced palpebral ptosis have been evaluated in mice. Some of them revealed interesting potencies since, although they are less active than the reference drugs, they exhibited a higher protective index. The experimental process involved the reaction of 6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5Quality Control of 6-Methoxybenzofuran-2-carbaldehyde)

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.Quality Control of 6-Methoxybenzofuran-2-carbaldehydeBenzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

《Synthesis of 2-amino-4-(2-benzofuryl)-Δ1-pyrrolines and study of their antiarrhythmic properties》 was written by Maillard, Jacques; Langlois, Michel; Tri, Vo Van; Guillonneau, Claude; Legeai, Jacques; Benharkate, Marguerite; Blozovski, Mladen. Quality Control of 6-Methoxybenzofuran-2-carbaldehyde And the article was included in European Journal of Medicinal Chemistry on August 31 ,1983. The article conveys some information:

2-Ethoxy-1-pyrrolines I (R = furyl, thienyl, benzofuryl, benzothienyl) were converted to amino analogs II (R1 = H, alkyl; R2 = H, alkyl, allyl, propargyl, CH2CH2OH, CH2CH2NMe2, phenethyl, Ph, OMe, OCH2Ph; or NR1R2 = pyrrolidino, morpholino, 4-methyl-1-piperazinyl), which showed antiarrhythmic activity. I (R = 2-benzofuryl) was heated with Me2NH.HCl in EtOH to give II (R = 2-benzofuryl, R1 = R2 = Me) hydrochloride. The results came from multiple reactions, including the reaction of 6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5Quality Control of 6-Methoxybenzofuran-2-carbaldehyde)

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.Quality Control of 6-Methoxybenzofuran-2-carbaldehydeBenzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

In 2017,Asian Journal of Organic Chemistry included an article by Reddy, Bhoomireddy Rajendra Prasad; Reddy, Peddiahgari Vasu Govardhana; Shankar, Muthukonda V.; Reddy, Bijivemula N.. Formula: C10H8O3. The article was titled 《CuI Supported on Protonated Trititanate Nanotubes: A Reusable Catalyst for the One-Pot Synthesis of Propargylamines via A3-Coupling》. The information in the text is summarized as follows:

CuI catalysts supported on protonated trititanate nanotubes (CuI/HTNT) were prepared and used as catalysts for the synthesis of propargylamines via A3 (aldehyde, amine and acetylene) coupling under solvent-free conditions. The results revealed that the CuI/HTNT with 5 wt % CuI had the best catalytic activity. The protocol provided access to a wide range of propargylamines in excellent yields (up to 98 %). The prepared catalysts were characterized by TEM, XRD, N2-adsorption desorption, EDS and ICP-MS anal. The catalyst was recovered by centrifugation and reused in further catalytic reactions, its activity remained largely unchanged for five successive runs. The results came from multiple reactions, including the reaction of 6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5Formula: C10H8O3)

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.Formula: C10H8O3Benzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

The author of 《The Vilsmeier reaction of fully conjugated carbocycles and heterocycles》 were Jones, Gurnos; Stanforth, Stephen P.. And the article was published in Organic Reactions (Hoboken, NJ, United States) in 1997. Formula: C10H8O3 The author mentioned the following in the article:

A review of the article The Vilsmeier reaction of fully conjugated carbocycles and heterocycles. In the experiment, the researchers used 6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5Formula: C10H8O3)

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.Formula: C10H8O3Benzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

HPLC of Formula: 53860-74-5On October 7, 2008 ,《New scaffolds for the design of selective estrogen receptor modulators》 was published in Organic & Biomolecular Chemistry. The article was written by Martin-Santamaria, Sonsoles; Rodriguez, Jose-Juan; de Pascual-Teresa, Sonia; Gordon, Sandra; Bengtsson, Martin; Garrido-Laguna, Ignacio; Rubio-Viqueira, Belen; Lopez-Casas, Pedro P.; Hidalgo, Manuel; de Pascual-Teresa, Beatriz; Ramos, Ana. The article contains the following contents:

In the present work we report the synthesis of four new ER ligands which can be used as scaffolds for the introduction of the basic side chains necessary for antiestrogenic activity. Affinities and agonist/antagonist characterization of the ligands for both ERα and ERβ have been determined in a competitive radioligand assay, and in an in vitro coactivator recruitment functional assay, resp. Mol. modeling techniques have been used in order to rationalize the exptl. results. Compound 2 is reported as a novel ERβ-agonist/ERα-antagonist. Two compounds show an interesting antitumor profile towards two pancreatic cancer cell lines and have been selected for in vivo assays. In addition to this study using 6-Methoxybenzofuran-2-carbaldehyde, there are many other studies that have used 6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5HPLC of Formula: 53860-74-5) was used in this study.

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.HPLC of Formula: 53860-74-5Benzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem