Day: March 7, 2022

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.885519-01-7,6-Bromo-4-chloro-1H-indole,as a common compound, the synthetic route is as follows.

885519-01-7, To a solution of 6-bromo-4-chloro-1H-indole (500 mg, 2.17 mmol), 1-methyl-4-(4,4,5,5-tetramcthyl-I ,3,2-dioxaborolan-2-yl)-1H-pyrazole (0.54 g, 2.60 mmol) and Na2CO3 (0.69 g,6.51 minol) in DME/T-120 (10 mL, 4: 1) was added bis(triphenylphosphine)palladium(II) dichloride (140 mg, 0.22 mmol). The mixture was heated to 120 C for 12 h under a nitrogen the mixture was extracted with EtOAc (10 mL x3). The combined organic layers werewashed with sat. aq. NaHCO3 (10 mL x 3), dried over anhydrous Na2SO4 and concentrated in vacuo. The crude residue was purified by silica gel chromatography (petroleum ether EtOAc= 3: 1) to give the title compound (0.38 g, 76%) as a light yellow solid.

885519-01-7 6-Bromo-4-chloro-1H-indole 24728099, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS, INC.; ROMERO, F. Anthony; MAGNUSON, Steven; PASTOR, Richard; TSUI, Vickie Hsiao-Wei; MURRAY, Jeremy; CRAWFORD, Terry; ALBRECHT, Brian, K.; COTE, Alexandre; TAYLOR, Alexander, M.; LAI, Kwong Wah; CHEN, Kevin, X.; BRONNER, Sarah; ADLER, Marc; EGEN, Jackson; LIAO, Jiangpeng; WANG, Fei; CYR, Patrick; ZHU, Bing-Yan; KAUDER, Steven; (0 pag.)WO2016/86200; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.343-93-1,1-(6-Fluoro-1H-indol-3-yl)-N,N-dimethylmethanamine,as a common compound, the synthetic route is as follows.

Step 2: In a round bottom flask with stir bar under nitrogen was placed 1 -(6-fluoro- 1 H-indol-3-yl)-N,N-dimethylmethanamine (21.03 g, 109.4 mmol). THF (200 rnl_) was added with stirring until all solid was in solution. In one portion iodomethane (17 ml_, 273.5 mmol) was added. Almost immediately a yellow precipitate formed. Stirring was continued overnight, after which time the solution was concentrated to dryness to provide 1-(6-fluoro-1 H-indol-3-yl)-N,N,N- trimethylmethanaminium iodide, which was used in the next step without further purification., 343-93-1

343-93-1 1-(6-Fluoro-1H-indol-3-yl)-N,N-dimethylmethanamine 2774471, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; WYETH; LUNDQUIST IV, Joseph Theodore; MAHANEY, Paige Erin; KIM, Younghee Callain; WO2010/36362; (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.1265231-91-1,3-(Dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile,as a common compound, the synthetic route is as follows.

5-Hydrazinyl-1H-benzo[d][1,2,3]triazole 5b (583mg, 1.98mmol) and 3-(dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile 1f (550mg, 1.45mmol) were suspended in 30mL of absolute ethanol, the reaction solution was heated to reflux for 4 hours. The reaction solution was diluted with 100mL of ethyl acetate, washed with saturated sodium bicarbonate solution (20mL) and then saturated sodium chloride solution (20mL), dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure to obtain (5-amino-1-(1H-benzo[d][1,2,3]triazol-5-yl)-1H-pyrazol-4-yl)(1-(phenylsulfonyl)-1H-indol-2-yl) methanone 5c (555mg, brown solid), yield: 89%. MS m / z (ESI): 483.8 [M + 1]

1265231-91-1, 1265231-91-1 3-(Dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile 68005411, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; Zhejiang Hisun Pharmaceutical Co., Ltd; CHEN, Lei; GUAN, Dongliang; BAI, Hua; YAN, Xing; MIAO, Shuai; ZHU, Songsong; (54 pag.)EP3339305; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.343-90-8,1-(5-Fluoro-1H-indol-3-yl)-N,N-dimethylmethanamine,as a common compound, the synthetic route is as follows.

Example 167; 2-(3-Fluoro-phenyl)-4-methyl-pyrimidine-5-carboxylic acid [5-fluoro-3- (2-pyridin-3-yl- ethyD-indol-l-yli- amide; Step 1 : A solution of 5-fluorogramine (576 mg, 3 mmol) and pyridine-3-carboxaldehyde (531 mg, 3 mmol) in MeCN (6 mL) is treated with Bu3P (1.12 mL, 4.5 mmol) and stirred at 900C for 24 h. The mixture is concentrated, filtered through a pad of silica gel eluting with 30% EtOAc in heptane to afford 5-fluoro-3-(2-pyridin-3-yl-vinyl)-lH-indole as a mixture of olefin isomers, which is used in the next step without further purification., 343-90-8

As the paragraph descriping shows that 343-90-8 is playing an increasingly important role.

Reference：
Patent; SANOFI-AVENTIS; WO2008/121670; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1145678-74-5,(1-Tosyl-1H-indol-4-yl)methanamine,as a common compound, the synthetic route is as follows.

Example 3: 1-U1H-indol-4-vhmethvn-9-f4.6-dimethylpyrimidin-2-yl)-1,9- diazaspiror5.51undecan-2-onea) tert-butyl 4-allyl-4-((1-tosvH H-indol-4-yl)methylamino)piperidine-1-carboxylateTo a stirred mixture of 1-Boc-piperidin-4-one (0.25 g, 1.256 mmol), 4 A molecular sieves (0.25 g), allyl boronic acid pinacol ester (0.255 g, 1.507 mmol) in toluene (10.0 mL), 1-tosyl- 1H-indol-4-yl)methanamine (0.45 g, 1.507 mmol) was added and the reaction mixture was heated to reflux for 16 h. The mixture was filtered through a pad of celite. The filtrate was concentrated under reduced pressure and the residue was purified by column chromatography (eluent: 10% ethyl acetate in hexane) to yield the title compound as a white solid (0.2 g, 70%). [LCMS RtE = 0.341 , [M+H]+ = 524.0]

1145678-74-5, As the paragraph descriping shows that 1145678-74-5 is playing an increasingly important role.

Reference：
Patent; NOVARTIS AG; BADIGER, Sangamesh; BEHNKE, Dirk; BETSCHART, Claudia; COTESTA, Simona; HINTERMANN, Samuel; OFNER, Silvio; PANDIT, Chetan; ROY, Bernard Lucien; WO2012/55888; (2012); 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