Category: 272-49-1

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.272-49-1,4-Azaindole,as a common compound, the synthetic route is as follows.

Intermediate 48: Synthesis of 3-(4-azetidin-l-ylcyclohex-l-en-l-yl)-li/-pyrrolo[3,2- b] pyridine1. Synthesis of 3-(l,4-dioxaspiro[4.51dec-7-en-8-yl)-lH-pyrrolo[3,2-blpyridine.Potassium hydroxide (41.0 mmol) was added to a mixture of 4-azaindole (13.5 mmol) and 1 ,4-cyclohexanedione monoethylene acetal (13.5 mmol) in methanol (30 mL) and the reaction mixture was heated at reflux for 4h. The reaction mixture was diluted with ice water(200 mL) and the precipitated solids were collected by filtration, washed with water, and air dried. The residue was purified by Flash chromatography (70/30 to 50/50 hexane/ethyl acetate) to provide 3-(l,4-dioxaspiro[4.5]dec-7-en-8-yl)-lH-pyrrolo[3,2-b]pyridine. Data: 1H NMR (CDCl3) 6 8.51 (dd, J= 4.7, 1.4, IH), 8.15 (br, IH), 7.63 (dd, J= 8.2, 1.4, IH), 7.36 (s, IH), 7.15(m, IH), 7.11 (dd, J = 8.2, 4.7, IH), 4.03 (s, 4H), 2.8-2.6 (m, 2H), 2.6-2.4 (m, 2H), 1.8-2.2 (m,2H).

272-49-1, 272-49-1 4-Azaindole 9226, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; MEMORY PHARMACEUTICALS CORPORATION; SCHUMACHER, Richard, A.; TEHIM, Ashok; XIE, Wenge; WO2010/24980; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.272-49-1,4-Azaindole,as a common compound, the synthetic route is as follows.

To a mixture of 1H-pyrrolo[3,2-b]pyridine (Purchased from Combi Blocks Inc.), (5 g) and DMF (100 mL) stirred under nitrogen at room temperature was added potassium hydroxide (9.02 g) followed by iodine (12.89 g) and the resulting mixture was stirred at room temperature for 1 h 5 min., then poured onto a mixture of Na2S2O5.5H2O (4.25 g), water (635 mL), and 28-30percent ammonium hydroxide (43 mL). The resultant mixture was cooled in an ice bath for 20 min, and the precipitate thus produced was filtered and washed with ice water then dried under vacuum to give the title compound (9.18 g). LCMS: m/z 245.39 [M+H]+. 1H NMR (400 MHz, DMSO-d6) ppm 7.17 (dd, J=8.1, 4.5 Hz, 1H) 7.72-7.87 (m, 2H) 8.38 (d, J=4.4 Hz, 1H) 11.74 (br. s., 1H)

272-49-1, As the paragraph descriping shows that 272-49-1 is playing an increasingly important role.

Reference£º
Patent; EISAI R&D MANAGEMENT CO., LTD.; PAYNE, Andrew; CASTRO PINEIRO, Jose Luis; BIRCH, Louise Michelle; KHAN, Afzal; BRAUNTON, Alan James; KITULAGODA, James Edward; SOEJIMA, Motohiro; WO2015/49574; (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.272-49-1,4-Azaindole,as a common compound, the synthetic route is as follows.

the mixture of the cyclic imine 3,4-dihydroisoquinoline (66 mg, 0.50 mmol);6,7-dihydrothieno[3,2-c]pyridine (51 mg, 0.38 mmol); 3,4-dihydro–carboline (63 mg, 0.38 mmol) or4,5-dihydro-3H-benz[c]azepine (55.3 mg, 0.38 mmol); and the electron-rich aromatic compound (7-, 6-,4-, or 5-azaindole (30 mg, 0.25 mmol)) were placed in a 10 mL pressurized reaction vial and heated ina microwave reactor, under the conditions given in Tables 1-3. In the case of 5-azaindole, 10 mol % ofp-TSA (4.3 mg, 0.025 mmol) as a catalyst was also added., 272-49-1

272-49-1 4-Azaindole 9226, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Belasri, Khadija; Fueloep, Ferenc; Szatmari, Istvan; Molecules; vol. 24; 19; (2019);,
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

272-49-1, 4-Azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Sodium hydride (19.1 mg, 0.48 mmol, 60percent> dispersion in mineral oil) was added portionwise to a solution of 4-azaindole (CAS: 272-49-1; 52 mg, 0.44 mmol) in DMF (4.12 mL) at rt. The resulting mixture was stirred at rt for 30 min. Then tert-butyl 3-(((methylsulfonyl)oxy)methyl)piperidine-l-carboxylate (CAS: 162166-99-6; 0.1 g, 0.34 mmol) was added and the mixture was further stirred at rt overnight. The mixture was poured in to ice and EtOAc was added. The organic layer was separated, washed with brine, dried over MgS04, filtered and concentrated in vacuo. The residue thus obtained was purified by flash column chromatography (silica; MeOH in DCM, 0/100 to 10/90) and the desired fractions were concentrated in vacuo to yield intermediate 68 as colorless oil (63 mg, 58percent yield)., 272-49-1

As the paragraph descriping shows that 272-49-1 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; BARTOLOME-NEBREDA, Jose, Manuel; TRABANCO-SUAREZ, Andres, Avelino; MARTINEZ VITURRO, Carlos, Manuel; TRESADERN, Gary, John; ALCAZAR-VACA, Manuel, Jesus; (126 pag.)WO2018/109198; (2018); 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

272-49-1, 4-Azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Azaindole (2.0 g, 16.93 mmol) was added to aluminum chloride (11.29 g, 85 mmol) in dry dichloromethane (85 mL) at 0 ¡ãC under argon atmosphere. After 30 mm ato ¡ãC, the mixture was warmed to room temperature and ethyl chlorooxoacetate (11.56 g,85 mmol) was added dropwise. The reaction mixture was stirred vigorously forovernight, then carefully ice was added. Adjust pH to 7 with 4 N NaOH then cold sat.NaHCO3 solution. The product was extracted with DCM 3 times, dried over Na2SO4,filtered, and concentrated to afford ethyl 2-oxo-2-(1H-pyrrolo[3,2-bjpyridin-3-yl)acetateas a yellow oily residue. After a washing with cold petroleum ether the title compound was obtained as a light yellow powder 280 mg (7.6percent). ESI-MS(-): MS m/z 217.1., 272-49-1

272-49-1 4-Azaindole 9226, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; MILLER, Michael Matthew; ALLEN, Martin Patrick; LI, Ling; BOWSHER, Michael S.; GILLIS, Eric P.; MULL, Eric; ZHAO, Qian; SUN, Li-Qiang; LANGLEY, David R.; SCOLA, Paul Michael; (214 pag.)WO2017/176608; (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