Category: 2795-41-7

2795-41-7, 6-Fluoroindole-3-carboxaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of glyoxalylhydrazide 18 (1.47mmol) and aldehyde 20 or 22 (1.47mmol) in ethanol (5mL) was refluxed for 6h. After completion of the reaction, ethanol was distilled off and the residue was taken into water (10mL) and allowed to stir at room temperature for 30min. The obtained suspension was filtered, washed with water and dried to obtain yellow solid ketohydrazide-hydrazones 21a-o and 23a-e in 88-96% yields., 2795-41-7

The synthetic route of 2795-41-7 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Tantak, Mukund P.; Klingler, Linus; Arun; Kumar, Anil; Sadana, Rachna; Kumar, Dalip; European Journal of Medicinal Chemistry; vol. 136; (2017); p. 184 – 194;,
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.2795-41-7,6-Fluoroindole-3-carboxaldehyde,as a common compound, the synthetic route is as follows.

General procedure: The van Leusen reaction was conducted as describedpreviously [37]. Aromatic aldehyde (3 mmol) was mixed withamine (15 mmol) in 20 mL of dry methanol. The reaction mixturewas left overnight to complete imine formation, although thisprocess can be monitored by this layer chromatography (TLC) (SiO2/CHCl3). Anhydrous K2CO3 (3 mmol) and TosMIC (tosylmethylisocyanide,3 mmol) were subsequently added. The mixture was stirredfor an additional 8 h, diluted with 50 mL of H2O, and extractedthree times with 20 mL of ethyl acetate. The combined extractswere washed twice with 20 mL of H2O, and once with 20 mL ofbrine, treated with anhydrous magnesium sulfate and evaporated.The final products were purified either by trituration under a 2:1hexane:isopropanol mixture, or chromatography on a short silicagelbed. The unreacted aldehydes were eluted with ethyl acetate orchloroform, and a mixture of AcOEt:MeOH or CHCl3:MeOH wasthen applied to elute the product.

2795-41-7, As the paragraph descriping shows that 2795-41-7 is playing an increasingly important role.

Reference：
Article; Hogendorf, Adam S.; Hogendorf, Agata; Popio?ek-Barczyk, Katarzyna; Ciechanowska, Agata; Mika, Joanna; Sata?a, Grzegorz; Walczak, Maria; Latacz, Gniewomir; Handzlik, Jadwiga; Kie?-Kononowicz, Katarzyna; Ponimaskin, Evgeni; Schade, Sophie; Zeug, Andre; Bijata, Monika; Kubicki, Maciej; Kurczab, Rafa?; Lenda, Tomasz; Staro?, Jakub; Bugno, Ryszard; Duszy?ska, Beata; Pilarski, Bogus?aw; Bojarski, Andrzej J.; European Journal of Medicinal Chemistry; vol. 170; (2019); p. 261 – 275;,
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.2795-41-7,6-Fluoroindole-3-carboxaldehyde,as a common compound, the synthetic route is as follows.

1.5 g 3-aldehyde-6-fluoroindole (ie intermediate I-1) was dissolved in isopropanol,Add 150 mg palladium on carbon and 3.2 g sodium borohydride,80 C reflux overnight.After TLC showed that the substrate disappeared,Filter to remove palladium carbon,After the filtrate is concentrated,Add water to quench excess sodium borohydride,Ethyl acetate extractionEach time 15ml,Extract 3 times.Organic layers merge,After drying over anhydrous sodium sulfate,Evaporated to drynessSilica gel column chromatography gave Intermediate I-2 (white solid, quantitative yield)., 2795-41-7

The synthetic route of 2795-41-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Chinese Academy Of Sciences Shanghai Pharmaceutical Institute; Hu Youhong; Geng Meiyu; Xing Weiqiang; Ding Jian; Ai Jing; (86 pag.)CN103664895; (2018); B;,
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.2795-41-7,6-Fluoroindole-3-carboxaldehyde,as a common compound, the synthetic route is as follows.

To a solution of 6-fluoro-1H-indole-3-carbaldehyde (0.97 g) in 90% formic acid (25 mL) were added hydroxylamine (0.65 g) and sodium formate (0.81g), and this mixture was stirred at 100C for 3 hours. After cooling to ambient temperature, water was added to this reaction mixture and the precipitated solid was collected by filtration, and washed with water, dried to give the title compound (0.57g).

2795-41-7, The synthetic route of 2795-41-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Kissei Pharmaceutical Co., Ltd.; EP2133332; (2009); 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

2795-41-7, 6-Fluoroindole-3-carboxaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To 15 mL of dichloromethane were added 6-fluoro-1H-indole-3-carbaldehyde (2.32 g, 14.2 mmol) and 4-dimethylaminopyridine (150 mg, 1.23 mmol) in turn. To the mixture was added dropwise di-tert-butyl dicarbonate (4.66 g, 21.3 mmol) at 0 C in a low temperature bath. After the addition, the mixture was reacted at 25 C for 24 hours. To the reaction mixure was added 50 mL of dichlormethane, and the resulting mixture was washed with saturated aqueous sodium bicarbonate (40 mL). The organic layer was dried over anhydrous sodium sulfate and filtered. The filtrate was concentrated in vacuo and the residue was purified by silica gel chromatography eluted with PE/EA(V/V)= 10/ito give the title compound as a white solid (3.31 g, 88.4%). The compound was characterized by the following spectroscopic data: ?H NMR (600 MHz, CDC13): 6 10.04 (s, 1H), 8.22-8.17 (m, 2H), 7.84 (d, J= 9.6 Hz, 1H), 7.10 (td, J= 9.0, 2.4 Hz, 1H), 1.69 (s, 9H).

2795-41-7, 2795-41-7 6-Fluoroindole-3-carboxaldehyde 262903, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; JIN, Chuanfei; ZHONG, Wenhe; ZHANG, Ji; GAO, Li; CHEN, Kangzhi; WO2015/90233; (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.2795-41-7,6-Fluoroindole-3-carboxaldehyde,as a common compound, the synthetic route is as follows.

2795-41-7, A. 6-Fluoro-3-(2-nitropropenyl)-1 H-indole was prepared by combining 6-fluoroindole-3-carboxaldehyde (485 mg, 2.97 mmol), nitroethane (6.0 mL), and ammonium acetate (250 mg, 3.27 mmol). The reaction solution was allowed to reflux 2 hours. The reaction solution was diluted with EtOAc (100 mL), washed with H20 (50 mL x 2), partitioned, dried over Na2SO4, filtered, and concentrated under reduced pressure to provide 560 mg (86 % yield) of 6-fluoro-3-(2-nitropropenyl)-1H- indole ; 1H NMR (CDCI3) b 11.03 (1H, brs), 8.41 (1H, s), 7.63 (1H, dd), 7.50 (1H, s), 7.06 (1H, dd), 6.92 (1H, t), 2.44 (3H, s); TLC (SiO2 plate, 100 % DCM) Rif-0 7

2795-41-7 6-Fluoroindole-3-carboxaldehyde 262903, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; X-CEPTOR THERAPEUTICS, INC.; WO2003/99821; (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

2795-41-7, 6-Fluoroindole-3-carboxaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,2795-41-7

41 mg of 6-fluoroindole and 42 mg of intermediate I-9 were dissolved in 10 ml of toluene,Add 0.6mg of palladium acetate under N2 protection.And 2.4 mg of Davephos (2-dicyclohexylphosphino-2′-(N,N-dimethylamine)-biphenyl),After stirring and dissolving,Added 32 mg of sodium tert-butoxide.Re-vacuum,Exchange nitrogen,And placed in a 90 C oil bath heated and stirred.After TLC showed that the substrate completely disappeared,The reaction was stopped and the reaction solution was cooled to room temperature.Infiltration is removed by suction filtrationThe filtrate was added with 30 ml of ethyl acetate.40ml water extraction,After the organic layer is washed once,dry,filter,80 mg of compound B-1 (white solid, yield 61.2%) was obtained.

The synthetic route of 2795-41-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Chinese Academy Of Sciences Shanghai Pharmaceutical Institute; Hu Youhong; Geng Meiyu; Xing Weiqiang; Ding Jian; Ai Jing; (86 pag.)CN103664895; (2018); B;,
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.2795-41-7,6-Fluoroindole-3-carboxaldehyde,as a common compound, the synthetic route is as follows.

Compound 1b (1.0 mmol, 177 mg) was added to a 25 mL sealed tube.Compound 2h (0.5 mmol, 81.6 mg), iodine simple substance (0.5 mmol, 127 mg),Pyridine (0.5 mmol, 39.6 mg) and 1,4-dioxane (2 mL),The reaction was then stirred in an oil bath at 110 C for 12 h. The reaction was quenched by the addition of 50 mL of water and extracted with ethyl acetate (50 mL×3).Washing with 10% Na2S2O3 solution and saturated brine,Dry over anhydrous sodium sulfate. Filter, spin dry,Separated by silica gel column(petroleum ether/ethyl acetate = 10/1, v/v)The product was obtained as a white solid 3s (123.7 mg, 68%)., 2795-41-7

The synthetic route of 2795-41-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Xinxiang Medical University; Gao Qinghe; Liu Xingxia; Yuan Huan; Wang Yakun; Tong Peiyuan; Shen Haotian; Zhang Zhiang; Zhang Weirong; Zhang Jixia; (22 pag.)CN108976198; (2018); 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

2795-41-7, 6-Fluoroindole-3-carboxaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a stirred solution of ketone 9b (50 mg, 0.34 mmol) andaldehyde (0.34 mmol) in anhydrous EtOH, piperidine (144.9 mg,1.72 mmol) was slowly added. After stirring for 10 h at 80 C, thereaction mixture was concentrated and extracted with CH2Cl2(3 20 mL). The combined organic layers were then washed withbrine, dried over anhydrous Na2SO4, and concentrated in vacuo toprovide the crude product, which was purified by column chromatography with petroleum/ethyl acetate (4:1) to give thecorresponding pure compounds 18a-i., 2795-41-7

The synthetic route of 2795-41-7 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Xu, Feijie; Li, Wenlong; Shuai, Wen; Yang, Limei; Bi, Yi; Ma, Cong; Yao, Hequan; Xu, Shengtao; Zhu, Zheying; Xu, Jinyi; European Journal of Medicinal Chemistry; vol. 173; (2019); p. 1 – 14;,
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.2795-41-7,6-Fluoroindole-3-carboxaldehyde,as a common compound, the synthetic route is as follows.

General procedure: To a solution of an appropriate indole, azaindole or alternative heterocycles (1.0 eq) and di-ferf-butyl dicarbonate (1eq. to 2 eq., more in particular 1.2 eq) in acetonitrile was added DMAP (0.1 to 0.5 eq. more in particular 0.1 eq). The reaction mixture was stirred overnight at room temperature. The reaction mixture was concentrated under reduced pressure. The residue was dissolved in dichloromethane and washed with a saturated sodium bicarbonate solution. The phases were separated. The aqueous phase was extracted with dichloromethane. The organic phases were combined, washed with a saturated ammonium chloride solution, water and brine, dried over magnesium sulfate, filtered and concentrated under reduced pressure. The BOC-protected compound was used in the next step without further purification.

2795-41-7, As the paragraph descriping shows that 2795-41-7 is playing an increasingly important role.

Reference：
Patent; KATHOLIEKE UNIVERSITEIT LEUVEN; BARDIOT, Dorothee; CARLENS, Gunter; DALLMEIER, Kai; KAPTEIN, Suzanne; McNAUGHTON, Michael; MARCHAND, Arnaud; NEYTS, Johan; SMETS, Wim; WO2013/45516; (2013); 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