Category: 387-44-0

Chemistry is traditionally divided into organic and inorganic chemistry. Recommanded Product: 387-44-0. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 387-44-0

Halogenated indoles eradicate bacterial persister cells and biofilms

The emergence of antibiotic resistance has necessitated new therapeutic approaches to combat recalcitrant bacterial infections. Persister cells, often found in biofilms, are metabolically dormant, and thus, are highly tolerant to all traditional antibiotics and represent a major drug resistance mechanism. In the present study, 36 diverse indole derivatives were investigated with the aim of identifying novel compounds that inhibit persisters and biofilm formation by Gram-negative Escherichia coli and Gram-positive Staphylococcus aureus. 5-Iodoindole and other halogenated indoles, 4-fluoroindole, 7-chloroindole, and 7-bromoindole, eradicated persister formation by E. coli and S. aureus, and 5-iodoindole most potently inhibited biofilm formation by the two bacteria. Unlike other antibiotics, 5-iodoindole did not induce persister cell formation, and 5-iodoindole inhibited the production of the immune-evasive carotenoid staphyloxanthin in S. aureus; hence, 5-iodoindole diminished the production of virulence factors in this strain. These results demonstrate halogenated indoles are potentially useful for controlling bacterial antibiotic resistance.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Recommanded Product: 387-44-0, you can also check out more blogs about387-44-0

Reference£º
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

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 387-44-0, name is 7-Fluoroindole, introducing its new discovery. Recommanded Product: 7-Fluoroindole

A catalyst-free system for 3-sulfenylation of free (N-H) indoles with mercaptobenzoic acid under alkaline conditions

We have developed a catalyst-free system for the 3-sulfenylation of free (N-H) indoles using mercaptobenzoic acid under alkaline conditions. The use of this system provides a green, convenient, and efficient method for the synthesis of 3-sulfenylindoles in good yields and with high selectivity. This simple synthesis process was carried out in a green solvent, isopropanol/H 2O, under atmospheric and catalyst-free conditions. The procedure is suitable for use with N-unprotected indoles. The Royal Society of Chemistry 2013.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 387-44-0 is helpful to your research. Recommanded Product: 7-Fluoroindole

Reference£º
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

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 387-44-0, name is 7-Fluoroindole, introducing its new discovery. name: 7-Fluoroindole

Suppression of fluconazole resistant Candida albicans biofilm formation and filamentation by methylindole derivatives

Candida albicans is an opportunistic fungal pathogen and most prevalent species among clinical outbreaks. It causes a range of infections, including from mild mucosal infections to serious life-threatening candidemia and disseminated candidiasis. Multiple virulence factors account for the pathogenic nature of C. albicans, and its morphological transition from budding yeast to hyphal form and subsequent biofilm formation is regarded as the most important reason for the severity of Candida infections. To address the demanding need for novel antifungals, we investigated the anti-biofilm activities of various methylindoles against C. albicans using a crystal violet assay, and the metabolic activity was assessed by using a 2,3-bis (2-methoxy-4-nitro-5-sulfo-phenyl)-2H-tetrazolium-5-carboxanilide reduction assay. Changes in biofilm morphologies and thicknesses were determined by confocal laser scanning microscopy and scanning electron microscopy, respectively. Of the 21 methylindoles tested, 1-methylindole-2-carboxylic acid (1MI2CA) at 0.1 mM (17.5 mug ml-1) and 5-methylindole-2-carboxylic acid (5MI2CA) at 0.1 mM effectively inhibited biofilm formation by C. albicans DAY185 and ATCC10231 strains. Moreover, 1MI2CA and 5MI2CA both effectively inhibited hyphal formation, and thus, improved C. albicans infected nematode survival without inducing acute toxic effects. Furthermore, our in silico molecular modeling findings were in-line with in vitro observations. This study provides information useful for the development of novel strategies targeting candidiasis and biofilm-related infections.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 387-44-0 is helpful to your research. name: 7-Fluoroindole

Reference£º
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

Chemistry is traditionally divided into organic and inorganic chemistry. 387-44-0. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 387-44-0

FUSED HETEROCYCLIC RING COMPOUND

A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy: wherein P: substituted 6-membered aromatic ring, Q: (substituted) 6-membered aromatic ring, A1: CR4aR4b, NR4c, O, S, SO or SO2 {R4a-4c: H etc.}, L1: (substituted) C1-5 alkylene, L2: a bond or (substituted) C1-3 alkylene, L3-4: (substituted) C1-3 alkylene, R1: H, X, CN, (substituted) hydrocarbon, (substituted) heterocycle or (substituted) OH, or (substituted) 4- to 8-membered (heterocyclic) ring together with A1, R2: H, CN, (substituted) hydrocarbon, and R3a: -COSRA1, (substituted) 5- or 6-membered aromatic ring {RA1: (substituted) hydrocarbon or (substituted) heterocycle}.

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 387-44-0 is helpful to your research. 387-44-0

Reference£º
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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.387-44-0,7-Fluoroindole,as a common compound, the synthetic route is as follows.

EXAMPLE 18 7-fluoro-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole Beginning with 2.0 gm (14.8 mMol) 7-fluoro-1H-indole and 4.6 gm (30.0 mMol) 4-piperidone hydrochloride monohydrate, 2.1 gm (66%) of the title compound were recovered as a white solid. m.p.=186-188 C. MS(FD): m/e=216 (M+) EA: Calculated for: C13 H13 N2 F: Theory: C, 72.20; H, 6.06; N, 12.95. Found: C, 72.41; H, 6.24; N, 13.09.

387-44-0, The synthetic route of 387-44-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Eli Lilly and Company; US5846982; (1998); A;,
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

387-44-0, 7-Fluoroindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,387-44-0

Example 37; 7-fluoro-1-f4-f4-fpyridin-2-yl)-1-fpyridin-3-yl)-1H-imidazol-2-yl)phenyl)-1H-indole; A mixture of 2-(2-(4-iodophenyl)-1-(pyridin-3-yl)-1H-imidazol-4-yl)pyridine (200 mg, 0.47 mmol), indole (76 mg, 0.56 mmol), CuI (134 mg, 0.7 mmol), K3PO4 (199 mg, 0.94 mmol) and fra?s-1,2-cyclohexanediamine (6 mg, 0.05 mmol) in p-dioxane (2 mL) was heated at 150 0C (bath) for 2h, filtered, concentrated, and the residue purified by SGC (0.5 and 1 % MeOH in DCM1 0.5 % NH4OH). Yield 80 mg, 39%. 1H NMR (CDCI3) delta 8.67 (m, 2H)1 8.57 (m, 1 H), 8.14 (d, 1H1 J = 7.9 Hz)1 7.93 (s, 1H), 7.77 (dt, 1H, J = 1.7, 7.7 Hz), 7.64 (m, 1H), 7.50 (m, 2H), 7.42-7.37 (m, 4H), 7.22-7.17 (m, 2H), 7.05 (m, 1H), 6.89 (dd, 1H1 J = 7.5, 13 Hz)1 6.68 (dd, 1H, J = 2.5, 3.3 Hz). MS (AP+) m/e 432 (MH+). IC50 = 30.8 ?M

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Reference£º
Patent; PFIZER PRODUCTS INC.; WO2008/4117; (2008); A1;,
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

387-44-0, 7-Fluoroindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Quinoline moiety – General Procedure Q In microwave vessel, quinoline (2.oeq) and indole (i.oeq) were mixed together and the system was sealed and placed under nitrogen, after a purge with vacuum/N2 (3 times). Then, HC1 solution 4 M in 1,4-dioxane (i.2eq) was added with the needle immersed in the mixture (exothermic reaction). The reaction mixture was heated with microwave during 2 h at 160 C. The reaction mixture was taken up with a minimum of MeOH and when the residue was dissolved, it was transferred in mixture of AcOEt and saturated NaHC03 solution. The resulting solution was extracted and the aqueous phase was washed with AcOEt (x2). The organic layers were combined, washed with o.oi M critic acid solution, saturated NaHC03 solution, dried over Na2S04 and concentrated to dryness under reduced pressure. Finally, the crude was purified by automated combi-flash to afford the good compound., 387-44-0

387-44-0 7-Fluoroindole 2774504, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; THE UNIVERSITY OF BRITISH COLUMBIA; SIMON FRASER UNIVERSITY; RENNIE, Paul; TCHERKASSOV, Artem; YOUNG, Robert, N.; ANDRE, Christophe, M.; WO2015/154169; (2015); A1;,
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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.387-44-0,7-Fluoroindole,as a common compound, the synthetic route is as follows.

Synthesis of 3-(7-fluoro-1H-indol-3-yl)-indan-1-one (Method 1) Triethylamine (4.5 mL; 32 mmol; 1.2 equiv.) was added to 3-bromo-indan-1-one (5.6 g; 27 mmol) in 100 mL THF at 0 C. and stirred 1 h at r.t. The reaction mixture was filtered to remove triethylammonium bromide and concentrated in vacuo to give inden-1-one. 7-Fluoroindole (3.3 g, 22 mmol) and Sc(OTf)3 (550mg, 5 mol %) were added to inden-1-one in 100 mL CH2Cl2 at 0 C. The reaction mixture was allowed to warm to room temperature over night. 100 mL ethyl acetate was added and the mixture was filtered through a silica gel plug and concentrated in vacuo. After flash chromatography (heptane/ethyl acetate, silica gel) 5.9 g 3-(7-fluoro-1H-indol-3-yl)-indan-1-one (82%) was isolated.

387-44-0, As the paragraph descriping shows that 387-44-0 is playing an increasingly important role.

Reference£º
Patent; H. Lundbeck A/S; US2008/58329; (2008); A1;,
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

387-44-0, 7-Fluoroindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

7-Fluoro-5-(piperazin-1-yl)-1H-indole To a mixture of 7-fluoro-1H-indole (18.5 g, 0.14 mol), borane trimethylamine complex (80 g, 1.1 mol) and 1,4-dioxane (700 mL) was, over a periode of 15 min, added a 37% aqueous HCl (80 mL) solution. The resulting solution reached a maximum temperature of 40 C., and the solution was subsequent stirred at room temperature for another 16 h. The mixture was boiled under reflux for 1 h, 6 M aqueous HCl (500 mL) was added, and the resuting mixture was boiled under reflux for another 15 min. The solution was concentrated at atmospheric pressure and poured onto a mixture of ice and brine. The aqueous phase was made alkaline by the use of 25% aqueous ammonia and extracted with ethyl acetate. The combined organic phase was dried (MgSO4), filtered and concentrated in vacuo. The residue was dissolved in a mixture of triethylamine (38 mL, 0.27 mol) and tetrahydrofuran (350 mL) and cooled to 10 C. Acetyl Chloride (11.2 g, 0.14 mol) was added to the mixture, which thereafter was filtered and concentrated in vacuo. The residue was purified by flash chromatography (ethyl acetate/heptane 50:50) to give 1-(7-fluoro-2,3-dihydro-1H-indol-1-yl-ethanone (16.7 g, 0.09 mol), which was dissolved in acetic acid (250 mL). To this mixture was added 100% nitric acid (5.8 ml, 0.14 mol) over a period of 5 min, and the resulting mixture was stirred at room temperature for 2 h. The reaction was not run to completion, and an additional amount of 6 mL of 100% nitric acid was added. Another 6 mL of 100% nitric acid was added and the mixture was stirred at room temperature for 16 h. The mixture was poured onto a mixture of ice and brine. The aqueous phase was made alkaline by the use of 25% aqueous ammonia and extracted with ethyl acetate. The combined organic phase was washed with brine, dried (MgSO4), filtered and concentrated in vacuo. The residue was crystallised from a mixture of ethyl acetate and 2-propanol to give 1-(7-fluoro-5-nitro-2,3-dihydro-1H-indol-1-yl)-ethanone (15.9 g), which was dissolved in methanol (500 mL). To this solution was added ammonium formate (44.4 g, 0.7 mol) and palladium (5 wt %, dry basis) on activated carbon (4.0 g), and the mixture was boiled under reflux for 30 min. The mixture was cooled in an ice bath, filtered and concentrated in vacuo. The residue was dissolved in methanol (100 mL) and ethyl acetate (500 mL), and ammonium formate precipitated out of solution and was removed by filtration. The mother liquor was concentrated in vacuo, and the residue was purified by flash chromatography (ethyl acetate/heptane 65:35) to give 1-(5-amino-7-fluoro-2,3-dihydro-1H-indol-1-yl)-ethanone (13.1 g, >91%). The compound was dissolved in methanol (350 mL), 28% aqueous sodium hydroxide (100 mL) and water (100 mL), and the resulting mixture was boiled under reflux for 4 h. The reaction mixture was concentrated to a volume of about 200 mL, and brine (1 L) was added. The aqueous phase was extracted with a mixture of ethyl acetate and tetrahydrofuran. The combined organic phase was washed with brine, dried (MgSO4), filtered and concentrated in vacuo to give 7-fluoro-2,3-dihydro-1H-indol-5-ylamine (11.0 g, 96%). This compound was dissolved in p-xylene (500 mL), and palladium (5 wt %, dry basis) on activated carbon (7.5 g) was added. The resulting mixture was boiled under reflux by the use of a Dean/Stark trap for 1.5 h, cooled and filtered. The filter cake was washed with ethyl acetate and tetrahydrofuran, and the organic phases were combined and concentrated in vacuo. The residue was purified by flash chromatography (ethyl acetate/heptane 50:50) to give 7-fluoro-1H-indol-5-ylamine (3.3 g, 29%). A further batch of 7-fluoro-1H-indol-5-ylamine was prepared (0.2 g), and the combined batch was used in the following. A mixture of N-benzyliminodiacetic (5.9 g, 0.027 mol), 1,1′-carbonyldiimidazole (9.0 g, 0.056 mol) and tetrahydrofuran (175 mL) was boiled under reflux for 30 min. To this solution was added a solution of 7-fluoro-1H-indol-5-ylamine (3.47 g, 0.023 mol) in tetrahydrofuran (75 mL) over a period of 1 h. The resulting mixture was boiled under reflux for 3 h and concentrated in vacuo to 50 mL. This solution was purified by flash chromatography (ethyl acetate/heptane 80:20) to give 4-benzyl-1-(7-fluoro-1H-indol-5-yl)piperazine-2,6-dione (7.8 g, 95%), which was dissolved in tetrahydrofuran (75 mL) and subsequently added drop wise to a solution of alane in tetrahydrofuran over 60 min at 5-10 C. The resulting mixture was stirred at 7 C. for 30 min and then quenched by addition of water (6.5 mL), 15% aqueous sodium hydroxide (3.25 mL) and water (16 mL). MgSO4 was added to the mixture, which was filtered and concentrated in vacuo. The residue was purified by flash chromatography (ethyl acetate/heptane 50:50) to give 5-(4-benzylpiperazin-1-yl)-7-fluoro-1H-indole (4.9 g, 63%). The alane was prepared as described in the following: Lithium aluminium hydride (3.23 g, 0.085 mol) was suspended in tet…, 387-44-0

387-44-0 7-Fluoroindole 2774504, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Bang-Andersen, Benny; Larsen, Krestian; Mork, Niels; US2007/43058; (2007); A1;,
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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.387-44-0,7-Fluoroindole,as a common compound, the synthetic route is as follows.,387-44-0

7-fluoro-1 H-indole (0.200 g),2,6-Bis (trifluoromethyl) benzoyl chloride (0.368 g)Was dissolved in dichloromethane (6 mL)After addition of zirconium (IV) chloride (0.517 g) under ice cooling,And the mixture was stirred at room temperature for 2 hours.Water was added to the reaction mixture under ice cooling, followed by extraction with ethyl acetate, and the organic layer was washed with saturated brine. The organic layer was dried over anhydrous sodium sulfate, concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (ethyl acetate / hexane) to give the title compound (0.234 g) as a colorless oil .

387-44-0 7-Fluoroindole 2774504, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; DAIICHI SANKYO COMPANY LIMITED; NAGAMOCHI, MASATOSHI; KOZAWA, YUJI; INAGAKI, HIROAKI; GOTANDA, KENTOKU; NOGUCHI, TETSUJI; TORIHATA, MUNEFUMI; YOSHINO, TOSHIHARU; ISOBE, TAKASHI; (113 pag.)JP2016/141632; (2016); A;,
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