Day: October 15, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.15317-58-5,1H-Indole-3-carbohydrazide,as a common compound, the synthetic route is as follows.

General procedure: 1H-Indole-3-carboxylate methylester 2 (1.0 mmol-equiv.) was refluxed with hydrazine hydrate(12.5 g, 0.25 M) in appropriate ethanol (30 mL) for 2 h. The progressof the reaction was monitored by TLC. After cooling the reactionmixture to room temperature, the mixtures were filtered to givewhite solid crude products without purification. Next, indolehydrazide(3, 1.0 mmol) in ethanol (30 mL) was added dropwiseinto the appropriate aldehyde (1.5 mmol-equiv.) and a few drops ofpropionic acid; the mixture was stirred and refluxed for 2.5 h. Aftercooling, the precipitates were filtered and washed several times bymethanol to yield the crystal substances 4aeu.

15317-58-5, As the paragraph descriping shows that 15317-58-5 is playing an increasingly important role.

Reference£º
Article; Ju, Zhiran; Su, Mingzhi; Hong, Jongki; La Kim, Eun; Moon, Hyung Ryong; Chung, Hae Young; Kim, Suhkmann; Jung, Jee H.; European Journal of Medicinal Chemistry; vol. 180; (2019); p. 86 – 98;,
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

348-36-7, Ethyl 5-fluoro-1H-indole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6.1. Ethyl 2-(ethoxycarbonyl)-5-fluoro-alpha-methylene-1H-indole-3-acetate. A solution of 37.2 g (180 mmol) of ethyl 5-fluoro-1H-indole-2-carboxylate, 25.8 g (222 mmol) of ethyl pyruvate and 31 ml of concentrated sulphuric acid in 400 ml of acetic acid is stirred for 20 h. The solvent is evaporated under reduced pressure, the residue is taken up in water and ethyl acetate, the organic phase is separated, washed with a dilute aqueous ammonia solution and then with a saturated aqueous sodium chloride solution and dried over sodium sulphate, and the solvent is evaporated under reduced pressure. 37.1 g (122 mmol) of solid product are obtained, which product is used as is in the following stage.

348-36-7, 348-36-7 Ethyl 5-fluoro-1H-indole-2-carboxylate 2727899, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Synthelabo; US6075021; (2000); 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

40913-43-7, 1-Ethyl-1H-indole-2-carbaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,40913-43-7

In two equal batches, 1,1 -dimethyl ethyl {(3R)-l-[(4-{[3-({[(9H-fluoren-9- ylmethyl)oxy]carbonyl}amino)propyl]amino}-3-nitrophenyl)carbonyl]-3- piperidinyl} carbamate (6 g, 9.32 mmol), l-ethyl-lH-indole-2-carbaldehyde (7.844 g, 27.96 mmol) and sodium hydrosulfite (4.868 g, 27.96 mmol) were combined in ethanol (40 mL) and water (20 mL) and heated in a Biotage Initiator microwave using initial high absorbtion setting to 100 C for 6 h. The reaction mixtures were combined and then partitioned between DCM (150 mL) and water (150 mL). The ethanol from the reaction mixture led to poor separation of the two layers, so the whole mixture was evaporated under vacuum – to the point where it was assumed most of the ethanol had evaporated and only the aqueous layer remained. The aqueous layer was then extracted with DCM (3 x 100 mL). The organics were combined, dried using a hydrophobic frit and evaporated under vacuum. The sample was loaded in dichlorom ethane and purified by Biotage SP4 (2 x SNAP 100 g silica) using a gradient of 50-100% cyclohexane-ethyl acetate. The appropriate fractions were combined and evaporated under vacuum to give the required product 1, 1 -dimethyl ethyl [(3R)-l-({2-(l- ethyl- 1 H-indol-2-yl)- 1 – [3 -( { [(9H-fluoren-9-ylmethyl)oxy] carbonyl } amino)propyl] – 1 H- benzimidazol-5-yl}carbonyl)-3-piperidinyl]carbamate (1.83 g, 2.386 mmol, 51.2 % yield) as an off- white foam.LCMS (Method B): Rt 1.37 min, MH+ 767.

As the paragraph descriping shows that 40913-43-7 is playing an increasingly important role.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; AMANS, Dominique; ATKINSON, Stephen, John; BARKER, Michael, David; CAMPBELL, Matthew; DIALLO, Hawa; DOUAULT, Clement; GARTON, Neil, Stuart; LIDDLE, John; RENAUX, Jessica, Fanny; SHEPPARD, Robert, John; WALKER, Ann, Louise; WELLAWAY, Christopher, Roland; WILSON, David, Matthew; (284 pag.)WO2016/185279; (2016); 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

875781-44-5, 5-Bromo-3-iodo-4,7-diazaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,875781-44-5

2-bromo-7-iodo-5-(phenylsulfonyl)-5H-pyrrolor3,2-blpyrazine (V-E-I); A mixture of (IV-E-I) (7.74 g, 23.9 mmol), PhSO2Cl (6.54 g , 4.73 mL , 37.04 mmol), Bu4NHSO4 (1.217 g , 3.584 mmol) and 50% aqueous NaOH (5 mL, 7.65 g, 95.6 mmol) in CH2Cl2 (100 mL) was stirred vigorously at RT for 3 h. A saturated solution of NaHCO3 (50 mL) was added and the mixture was extracted with CH2Cl2 (4 x 50 mL). The combined organic extracts were dried (MgSO4), concentrated, and the residue was triturated with MeOH (100 mL). The solid was filtered off and dried in vacuo to afford V-E-I (9.34 g, 85%) as yellow solid. 1H NMR (400 MHz, CDCl3) delta 7.49-7.60 (m, 2H), 7.62-7.73 (m, IH), 8.15 (d, J0.51, IH), 8.16-8.21 (m, 2H), 8.44 (d, J0.38, IH). MS (ES) M+ m/e = 464.

The synthetic route of 875781-44-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; EISAI R & D MANAGEMENT CO. LTD; GRACZYK, Piotr; BHATIA, Gurpreet, Singh; WO2010/15803; (2010); 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

51843-24-4, 1-(5-Chloro-1H-indol-3-yl)ethanone is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

51843-24-4, General procedure: The substituted 1-(1H-indol-3-yl)ethanone (1 mmol), together with the respective benzaldehyde (1 mmol), malononitrile (1 mmol) and ammonium acetate (8 mmol) were dissolved in toluene (30 mL) and heated to reflux for 8 h. The solvent was removed under reduced pressure and absolute ethanol was added to the residue. The precipitate was collected by filtration and purified by silica gel column chromatography to give the desired product.

51843-24-4 1-(5-Chloro-1H-indol-3-yl)ethanone 2762971, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Zhang, Fan; Zhao, Yanfang; Sun, Li; Ding, Lu; Gu, Yucheng; Gong, Ping; European Journal of Medicinal Chemistry; vol. 46; 7; (2011); p. 3149 – 3157;,
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

17422-32-1, 5-Chloroindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[1238] Preparation of DJ-2 . To a solution of DJ-1 (1 g, 6.60 mmol, 1 eq) in DMF (10 mL) was added KOH (925.27 mg, 16.49 mmol, 2.5 eq) followed by dropwise addition of I2 (1.67 g, 6.60 mmol, 1.33 mL, 1 eq) in DMF (10 mL). The mixture was stirred at 10C. for 2 h to give a red-brown solution. LCMS showed the reaction was completed. The reaction mixture was quenched with H2O (60 mL) and extracted with MBTE (20 mL3). The organic layers were dried over Na2SO4 and concentrated to give the crude product, which was used for next step without further purification., 17422-32-1

17422-32-1 5-Chloroindole 87110, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Ferro Therapeutics, Inc.; Jiang, Chun; Chen, Ruihong; Pandey, Anjali; Kalita, Biswajit; Duraiswamy, Athisayamani Jeyaraj; (293 pag.)US2019/263802; (2019); 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.885520-70-7,4-Bromo-6-fluoro-1H-indole,as a common compound, the synthetic route is as follows.

885520-70-7, To a solution of 4-bromo-6-fluoro-indole (2 g, 9.38 mmol) in anhydrous tetrahydrofuran (30 mL) cooled in an ice bath was added sodium hydride (0.452 g, 11.3 mmol, 60percent in mineral oil). The reaction mixture was stirred under nitrogen for 10 min before benzenesulfonyl chloride (1.44 mL, 11.3 mmol) was added. The black solution was allowed to warm to room temperature over 4 h. TLC and LCMS indicated completion of the reaction. Saturated aqueous ammonium chloride solution was added slowly, and the resulting solution was extracted with ethyl acetate (2*). The combined organic phases were washed with brine, dried over anhydrous sodium sulfate, filtered, and concentrated in vacuo. The crude solid was triturated with ethanol. The resulting beige solid was collected by filtration to give 4-bromo-6-fluoro-1-(phenylsulfonyl)-1H-indole (2.6 g, 79percent yield).

The synthetic route of 885520-70-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PMV Pharmaceuticals, Inc.; Vu, Binh; Dominique, Romyr; Li, Hongju; (222 pag.)US2017/240525; (2017); 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

6146-52-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.6146-52-7,5-Nitroindole,as a common compound, the synthetic route is as follows.

General procedure: Phosphorous oxychloride (2 mmol) was added dropwise to dimethylformamide (3 mL) cooled under ice-bath and allowed to stir for 30 min. A solution of indoles 4a-4h or azaindole 5 (1 mmol) in DMF (5 mL) was added dropwise for 5 min at 0 oC. The mixture was further allowed to stir for 3 h at 90-100 oC. Reaction mixture was cooled to room temperature and poured into crushed ice. Excess POCl3 was quenched with 1 N NaOH and left overnight at room temperature. Ice-cold reaction mixture was then extracted (50 mL ¡Á 3) with EtOAc. Combined organic layer was concentrated on rotary evaporator and crude products were purified by silica gel (No.100-200) column chromatography to get indole-3-carboxaldehydes 1a-1h or 6 in 60-80% yield.

The synthetic route of 6146-52-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Yadav, Rammohan R.; Battini, Narsaiah; Mudududdla, Ramesh; Bharate, Jaideep B.; Muparappu, Nagaraju; Bharate, Sandip B.; Vishwakarma, Ram A.; Tetrahedron Letters; vol. 53; 17; (2012); p. 2222 – 2225;,
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

40047-23-2, 6-Hydroxyindole-2-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

a 1-(4-Benzylpiperidine-1-yl)-1-(6-hydroxy-1H-indole-2-yl)methanone A mixture of 5.0 g (28.2 mmol) of 6-hydroxy-indole-2-carboxylic acid [J. Chem. Soc. 1605-1608. (1948)], 4.4 ml (31.6 mmol) of triethylamine, 5.0 g (28.5 mmol) of 4-benzylpiperidine, 12.0 g (31.6 mmol) of HBTU (Advanced Chem. Tech.) and 50 ml of dimethylformamide is stirred at room temperature for 6 h. The precipitated product is filtered off and recrystallized from ethanol to yield 6.75 g (71percent) of the title compound. Mp: 214-215¡ã C. (ethanol).

40047-23-2, The synthetic route of 40047-23-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; RICHTER GEDEON VEGYESZETI GYAR RT.; US2003/199552; (2003); 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.1074-88-0,1H-Indole-7-carbaldehyde,as a common compound, the synthetic route is as follows.

EXAMPLE I 1-methyl-1H-indole-7-carbaldehyde 20 g 1H-indole-7-carbaldehyde are dissolved in 160 ml N,N-dimethylformamide and combined batchwise with 15.5 g potassium-tert.-butoxide under argon. After the addition has ended the mixture is left for 20 minutes with stirring and then 8.7 ml methyl iodide are added dropwise. Then the mixture is left for 12 hours at ambient temperature with stirring and then distributed between water and ethyl acetate. The aqueous phase is twice extracted with ethyl acetate and the combined organic phases are washed with saturated aqueous sodium chloride solution. After drying with magnesium sulphate the solvents are eliminated in vacuo. The residue is extracted from water. The solid thus obtained is suction filtered and dried in vacuo. Yield: 20 g (91% of theory) Mass spectrum (ESI+): m/z=160 [M+H]+

1074-88-0, As the paragraph descriping shows that 1074-88-0 is playing an increasingly important role.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; US2011/269737; (2011); 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