Day: March 24, 2022

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.676273-39-5,3-Iodo-1-tosyl-1H-indole-5-carbonitrile,as a common compound, the synthetic route is as follows.

676273-39-5, Preparation of compound 69c: N’-hydroxy-3-iodo-l-tosyl-l/7-indole-5- carboximidamideTo a suspension of 3-iodo-l-tosyl-l//-indole-5-carbonitrile (1 g, 2.37 mmol) in EtOH (10 mL) was added Et3N (1.65 mL, 11.87 mmol) followed by NH2OH.HCl (410 mg, 5.93 mmol) and the reaction was stirred for 48 h at RT. The solvent was removed in vacuo and the residue was treated with H20 (10 mL) and extracted with EtOAc (25 mL). The aqueous layer was extracted with EtOAc (25 mL). The combined organic layers were dried over anhydrous Na2S04, filtered and concentrated. The residue was further triturated with n-pentane to give N’-hydroxy-3-iodo-l-tosyl-l//-indole-5- carboximidamide (950 mg, 88.7%o) as an off brown solid. MS (ESI, pos. ion) m/z: 455.8; .H NMR (400MHz, CDC13): delta 7.99 (d, J=8.8Hz, 1H), 7.84-7.73 (m, 4H), 7.68 (d, J=8.4Hz, 1H), 7.63-7.61 (m, 1H), 7.31-7.24 (m, 1H), 4.92 (brs, 2H), 3.14-3.09 (m, 1H), 2.36 (s, 3H).

The synthetic route of 676273-39-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; AMGEN INC.; WANG, Hui-Ling; CEE, Victor, C.; HERBERICH, Bradley, J.; JACKSON, Claire, L., M.; LANMAN, Brian, Alan; NIXEY, Thomas; PETTUS, Liping, H.; REED, Anthony, B.; WU, Bin; WURZ, Ryan; TASKER, Andrew; WO2012/129338; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.399-67-7,7-Fluoro-1H-indole-2-carboxylic acid,as a common compound, the synthetic route is as follows.,399-67-7

To a solution of 7-fluoro-1H-indole-2-carboxylic acid (78 mg, 0.435 mmol), (S)-2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)-5 -(piperidin-3-yl)benzofuran-3 -carboxamide (100 mg, 0.218 mmol) in DCM (1 ml) was added N,N-diisopropylethylamine (169 mg, 1.306 mmol), and the reaction mixture stirred for 5 mm at RT. Then 2,4,6-tripropyl-1,3,5,2,4,6- trioxatriphosphinane 2,4,6-trioxide (415 mg, 0.653 mmol) was added to the reaction mixture and stirred at RT overnight under N2 protection. The reaction mixture was concentrated under vacuum,then applied onto a silica gel column and eluted with 0-30% MeOH/EtOAc. This resulted in 78 mg (58%) of (S)-5-(1 -(7-fluoro- 1 H-indole-2-carbonyl)piperidin-3-yl)-2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)benzofiiran-3-carboxamide as white solid. LC-MS (ES, mlz) C32H30F2N4055: 620; Found: 621 [M+H]b.

399-67-7 7-Fluoro-1H-indole-2-carboxylic acid 3159626, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; MERCK SHARP & DOHME CORP.; HE, Shuwen; LAI, Zhong; DAI, Xing; XIAO, Dong; LONDON, Clare; ZORN, Nicolas; NARGUND, Ravi; PALANI, Anandan; MCCOMAS, Casey C.; LI, Peng; PENG, Xuanjia; SOLL, Richard; WO2014/205592; (2014); 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

14618-45-2, 3-(Trifluoroacetyl)indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

14618-45-2, To a solution of this compound (11 g, 50 mmol) in 100 mL acetone were added MeI (10 mL, 150 mmol) and potassium carbonate (18 g), and stirring was continued at RT for 2 h. Acetone was removed in vacuo. Water and methylene chloride were added to the residue. The organic layer was separated, washed with brine, dried and concentrated in vacuo to yield crude 1-methyl-3-trifluoroacetyl-1H-indole.

The synthetic route of 14618-45-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Monsanto Company; US5994270; (1999); 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

1265231-91-1, 3-(Dimethylamino)-2-(1-(phenylsulfonyl)-1H-indole-2-carbonyl)acrylonitrile is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1265231-91-1, Step 1: Synthesis of [5-amino-1-(2-methyl-1H-benzimidazol-5-yl)-1H-pyrazol-4-yl]-(1-benzenesulfonyl-1H-indol-2-yl)-methanone (1001) (2-Methyl-1H-benzimidazol-5-yl)-hydrazine dihydrochloride (830 mg) was added to an ethanol solution (15 ml) of crude 2-(1-benzenesulfonyl-1H-indole-2-carbonyl)-3-dimethylamino acrylonitrile (1.17 g). The reaction mixture was heated with stirring under reflux for four hours. After cooling to room temperature, the mixture was allowed to stand at room temperature. The precipitated solid was collected by filtration, and washed with ethanol to give [5-amino-1-(2-methyl-1H-benzimidazol-5-yl)-1H-pyrazol-4-yl]-(1-benzenesulfonyl-1H-indol-2-yl)-methanone was obtained as a yellow solid (1.5 g, with a two-step yield of 91%). 1H-NMR (DMSO-D6) delta: 8.15-8.13 (2H, m), 8.02 (1H, dd, J = 8.4, 0.8 Hz), 7.97 (1H, d, J = 2.0 Hz), 7.92 (1H, d, J = 8.8 Hz), 7.87 (1H, s), 7.76-7.62 (5H, m), 7.49-7.45 (1H, m), 7.36-7.26 (4H, m), 2.82 (3H, m) ESI (LC-MS positive mode) m/z 497 [(M+H)+]

As the paragraph descriping shows that 1265231-91-1 is playing an increasingly important role.

Reference：
Patent; Chugai Seiyaku Kabushiki Kaisha; F.Hoffmann-La Roche AG; EP2471786; (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

434958-85-7, N-Boc-5-Hydroxyindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

100 mg (0.4 mmol) of 5-hydroxy-1-tert-butyl ester-1H-indole (a) was dissolved in 1 ml of DMF, and 0.5 ml (4 mmol) of p-fluoroacetophenone and 0.96 g (0.8 mmol) were added.Potassium tert-butoxide, stirred at 100 C for 7 hours, diluted with water, extracted with EA,Wash with saturated sodium chloride, dry over anhydrous sodium sulfate, concentrate under reduced pressure, and thenPE: EA=150:1 to get an oil,The yield was 46%.

434958-85-7, The synthetic route of 434958-85-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Tianjin University of Science and Technology; Yu Peng; Guo Na; Lv Hongbin; Fu Ying; Teng Yuou; Wang Dong; (32 pag.)CN110229091; (2019); 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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.171879-99-5,4-Chloro-6-methyl-7-azaindole,as a common compound, the synthetic route is as follows.

To a 0 C suspension of 4-chloro-6-methyl-1H-pyrrolo[2,3-b]pyridine (1.7 g, 10mmol) in N,N-dimethylformamide (20 mL) was added potassium hydroxide (1.14 g, 20.3 mmol), followed by iodine (2.54 g, 10.0 mmol). The reaction mixture was allowed to warm to room temperature and stir for 4 hours, whereupon it was diluted with water and filtered, to afford the product as a white solid. Yield: 1.6 g, 5.5 mmol, 55%. H NMR (400 MHz, CD3OD) oe 7.47 (s, 1 H), 7.04 (s, 1 H), 2.54 (s, 3H)., 171879-99-5

As the paragraph descriping shows that 171879-99-5 is playing an increasingly important role.

Reference：
Patent; PFIZER INC.; GALATSIS, Paul; HAYWARD, Matthew Merrill; KORMOS, Bethany Lyn; WAGER, Travis T.; ZHANG, Lei; HENDERSON, Jaclyn Louise; KURUMBAIL, Ravi G.; VERHOEST, Patrick Robert; STEPAN, Antonia Friederike; WO2015/92592; (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

5192-03-0, 1H-Indol-5-amine is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Using procedure A: 2-Amino-3,5-dibromo-pyrazine (100 mg) and 5-aminoindole (200 mg) yielded 150 mg of a 1 :1 mixture of 5-aminoindole and the desired product MS m/z 303 [M + H]+ which was used without further purification or characterization.; Procedure A:General procedure for SNAgamma on 2-amino-3,5-dibromo-pyrazine2-Amino-3,5-dibromo-pyrazine, triethylamine (3 equiv) and the appropiate amine or alcohol (3 equiv) were dissolved in 4 mL water and the resulting mixture was heated to 195 0C for 1 hour. Water and ethyl acetate were added and the phases separated. The water phase was extracted once more with ethyl acetate. The combined organic phases were washed (water and brine) and concentrated to yield a crude mixture of product and unre- acted amine or alcohol. This crude mixture was used without further purification or characterization in the subsequent Suzuki reaction.

5192-03-0, The synthetic route of 5192-03-0 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BIOVITRUM AB (publ); WO2009/95399; (2009); A2;,
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.31241-19-7,5-Methoxy-2,3,3-trimethyl-3H-indole,as a common compound, the synthetic route is as follows.

General procedure: In parallel, substituted hydrazines 1 (4.0 g, 22.25 mmol) were reacted with 3-methylbutanone(3 mL, 28.04 mmol) in acetic acid and heated to a 100 C for 24 h. The solution was then neutralizedusing sodium bicarbonate and extracted using dichloromethane; affording substituted indolenineheterocycles 2 which was dried under reduced pressure. The heterocycles 2 were then reacted withan alkyl halide in acetonitrile at 100 C for 12-18 h. The quaternary ammonium salts 3 were precipitatedwith diethyl ether, and collected.

31241-19-7, The synthetic route of 31241-19-7 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Levitz, Andrew; Marmarchi, Fahad; Henary, Maged; Molecules; vol. 23; 2; (2018);,
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.165250-69-1,4-Methyl-5-nitro-1H-indole,as a common compound, the synthetic route is as follows.

5-(4-Methyl-5-nitroindol-3-ylmethyl)-2,2-dimethyl-1,3-dioxane-4,6-dione An adaption of the procedure of Flaugh was used. Thus, a solution of 4-methyl-5-nitroindole (0.880 g, 5.00 mmol), Meldrum’s acid (0.864 g, 6.00 mmol), 37% aqueous formaldehyde (0.5 mL, 6.0 mmol) and D,L-proline (0.029 g, 0.25 mmol) in 25 mL of acetonitrile was stirred at room temperature for 72 h. The resulting yellow slurry was stored at -20 C. and then the cold mixture was filtered. The filtercake was washed with cold acetonitrile and ether, and then it was dried in vacuo to give the title compound (1.055 g, 64%) as a canary-yellow solid, mp 196-198 C. (dec): IR (KBr) 3338, 1782, 1742 cm-1; 1 H NMR (DMSO-d6, 200 MHz) delta 11.46 (br s, 1H), 7.61 (d, J=8.9 Hz, 1H), 7.32 (d, J=8.9 Hz, 1H), 7.25 (d, J= 2.4 Hz, 1H), 4.74 (t, J=5.0 Hz, 1H), 3.64 (d, J=4.9 Hz, 1H), 2.80 (s, 3H), 1.84 (s, 3H), 1.69 (s, 3H). Anal. Calcd for C16 H16 N2 O6: C, 57.83; H, 4.85; N, 8.43. Found: C, 57.42; H, 4.68; N, 8.52., 165250-69-1

The synthetic route of 165250-69-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Bristol-Myers Squibb Company; US5521188; (1996); 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

16732-69-7, Ethyl 7-bromo-1H-indole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1 S-Benzoyl^-bromo-lH-indole^-carboxylic acid ethyl ester To a solution of 7-bromo-lH-indole-2-carboxylic acid ethyl ester (2.04 g, 7.6 mmol) in 1,2- dichloroethane (60 ml) were added AICI3 (2.0 g, 15.0 mmol) and benzoic anhydride (3.45 g, 15.2 mmol). After heating at 9O0C for 2 hours, the reaction mixture was poured into a mixture OfEtOAcZH2O. The organic fraction was separated and washed with water and brine. After drying over MgSO4, the organic fraction was concentrated in vacuo and the resulting residue was purified by flash chromatography to give b-Benzoyl-7-bromo-lH- indole -2 -carboxylic acid ethyl ester as yellow solid (-100%). MS: (M+H)+ 374.1.

16732-69-7, As the paragraph descriping shows that 16732-69-7 is playing an increasingly important role.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; WO2008/55808; (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