Indole Building Blocks

24985-85-1, Ethyl 5-hydroxyindole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 5-hydroxyindole-2-carboxylic acid ethyl ester (14.2 g, 68.5 mmol) in DMF (150 mL) was added cesium carbonate (26.8 g, 82.3 mmol). The resulting mixture was stirred at room temperature for 20 min followed by the addition of allyl bromide (5.94 mL, 68.5 mmol). The reaction mixture was stirred at room temperature for 24 h. The reaction was diluted with ethyl acetate, washed with H2O, brine and dried (Na2SO4). The solvent was removed in vacua and the resulting crude product was purified by flash column chromatography on silica gel (0-20% EtOAc/hexanes) to give the desired material as solid (8.9 g, 52%). LC/MS (ES+) m/e 248 [M+H]+.

24985-85-1, 24985-85-1 Ethyl 5-hydroxyindole-2-carboxylate 90677, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; SmithKline Beecham Corporation; US6670388; (2003); B1;,
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

10242-01-0, 5-Methoxy-1H-indole-3-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

10242-01-0, General procedure: 60% NaH (0.91 g, 22.8 mmol) was added in portions to a solution of 1b-h (11.2 mmol) in dry DMF (35 mL) at 0-5 C. After addition, the mixture was stirred for 30 min. Iodomethane (33.6 mmol) was then added at 0-5 C and stirred for 2 h at room temperature. The mixture was then poured into H2O (120 mL) and the resulting solution was extracted with ethyl acetate (50 mL ¡Á 3). The organic phase was combined and washed with brine (150 mL ¡Á 3), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The obtained residue was purified by flash column chromatography on silica gel to afford 2b-h.

As the paragraph descriping shows that 10242-01-0 is playing an increasingly important role.

Reference£º
Article; Hu, Yuanyuan; Ruan, Wenchen; Gao, Anhui; Zhou, Yubo; Gao, Lixin; Xu, Meng; Gao, Jianrong; Ye, Qing; Li, Jia; Pang, Tao; Pharmazie; vol. 72; 12; (2017); p. 707 – 713;,
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

101774-27-0, 6-Bromo-1H-indole-3-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a 250 mL round bottom Hask was added 6-bromo-l H-indole-3-carboxylic acid ASa(5 g, 20.83 mmol, 1.0 equiv.), N,N-dimethylformamide (150 mL), Mel (5.9 g), andsodium hydride (3.5 g, 145.83 mmol, 7.0 equiv.). The resulting mixture ‘.Vas stirred at 10-25 oc for l h, a.nd then diluted with 1500 mL ofH?O. The aqueous mixture was extracted15 with ethyl acetate (200 mL x 3) and the combined organic layers were dried over anhydrousmagnesium sulfate, filtered, and concentrated in vacuo. The cmde product was purified byre-crystallization from PE. The solids were collected by filtration to yield 3.5 g (63%) ofmethyl 6-brorno-l-methyl-l H-indole-3-carboxylate A-8b a.s a light yellow solid.

101774-27-0, The synthetic route of 101774-27-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARDELYX, INC.; CHAO, Jianhua; JAIN, Rakesh; HU, Lily; LEWIS, Jason Gustaf; BARIBAULT, Helene; CALDWELL, Jeremy; (582 pag.)WO2018/39386; (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.1201-26-9,3-Indolylacetone,as a common compound, the synthetic route is as follows.

[0570] Asymmetric reduction applying transaminase TA-P2-A07 was performed in buffer; iso-propyl amine and organic co-solvents such as DMSO or Acetonitrile on 5 g scale. Compound (XXI) was converted to compound (3) as described herein at a degree above 95% with an enantiomeric excess (EE) above 99% after 1 day.

1201-26-9, As the paragraph descriping shows that 1201-26-9 is playing an increasingly important role.

Reference£º
Patent; GENENTECH, INC.; F. HOFFMANN-LA ROCHE AG; CHUNG, Cheol Keun; XU, Jie; IDING, Hans; CLAGG, Kyle; DALZIEL, Michael; FETTES, Alec; GOSSELIN, Francis; LIM, Ngiap-Kie; ZHANG, Haiming; CHAKRAVARTY, Paroma; NAGAPUDI, Karthik; ROBINSON, Sarah; (241 pag.)WO2019/245974; (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

902772-13-8, 5-Bromo-1H-indole-2-carbonitrile is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

902772-13-8, Anhydrous CH2Cl2 (270 mL), Et3N (4.86 mL, 34.7 mmol) and pyridine (2.82 mL, 34.7 mmol) were added to 5-bromoindole-2-carbom’trile (3.83 g, 17.3 mmol; see step (b) above), Cu(OAc)2 (6.29 g, 34.7 mmol), 3 A molecular sieves (ca. 7 g) and4-cyclopentyloxyphenylboronic acid (7.15 g, 34.7 mmol). The mixture was stirred vigorously at rt for 72 h and filtered through Celite. The solids were washed withEtOAc, and the combined filtrates concentrated and purified by chromatography to afford the sub-title compound (3.87 g, 59%).

902772-13-8 5-Bromo-1H-indole-2-carbonitrile 68473340, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; BIOLIPOX AB; WO2006/77367; (2006); 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

942-26-7, 5-Chlorotryptamine hydrochloride is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

942-26-7, General procedure: Commercial tryptamine hydrochloride (4.9 g, 24.9 mmol, 1 eq) and glyoxylic acid (2.6 g, 27.4 mmol, 1.1 eq) were dissolved in 78 mL H2O,and then the solution of KOH (1.38 g, 24.9 mmol, 1 eq) in 6 mL H2O was added dropwise. The mixture was stirredfor 1h and the white precipitate was collected by filtration. The precipitate was dissolved in 78 mL H2O and thesolution was added conc. HCl (6.6 mL) at room temperature. After stirring for one hour under reflux, the solutionwas added 6.6 mL conc. HCl again and stirred for another 0.5 h under reflux. After cooling to r.t., the light-greencrystal was obtained and collected by filtration and then dissolved in 78 mL H2O. The solution was basified by 20%KOH until pH > 13, and the white precipitate was filtered off and washed with water three times to the titlecompound S16a (3.1 g, 73%).

942-26-7 5-Chlorotryptamine hydrochloride 2827494, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Zheng, Hongbo; Li, Lin; Sun, Bin; Gao, Yun; Song, Wei; Zhao, Xiaoyu; Gao, Yanhui; Xie, Zhiyu; Zhang, Nianzhao; Ji, Jianbo; Yuan, Huiqing; Lou, Hongxiang; European Journal of Medicinal Chemistry; vol. 150; (2018); p. 30 – 38;,
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.348640-06-2,4-Bromo-7-azaindole,as a common compound, the synthetic route is as follows.

348640-06-2, A solution of 4-bromo-1H-pyrrolo[2,3-b]pyridine (10.0 g, 0.0508 mol) in DMF (40 mL) was cooled under nitrogen to 0 C. Sodium hydride (3.0 g, 0.075 mol) was added portionwise. The reaction was stirred for 1 hour. To this mixture, [2-(trimethylsilyl)ethoxy]methyl chloride (10.8 mL, 0.061 mol) was added slowly. After being stirred at 0 C. for 1 hour, the reaction was quenched with water and extracted with EtOAc twice. The combined extracts were washed with water, brine, dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure. The residue was purified by silica gel chromatography, eluting with 0-25% EtOAc/hexanes to afford 15.7 g (94.5%) of the desired product as a yellowish oil. LC/MS found: 327.1, 329.1 (M+H)+.

As the paragraph descriping shows that 348640-06-2 is playing an increasingly important role.

Reference£º
Patent; Huang, Taisheng; Xue, Chu-Biao; Wang, Anlai; Kong, Ling Quan; Ye, Hai Fen; Yao, Wenqing; Rodgers, James D.; Shepard, Stacey; Wang, Haisheng; Shao, Lixin; Li, Hui-Yin; Li, Qun; US2011/224190; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.143612-79-7,3-(4-Chlorobutyl)-1H-indole-5-carbonitrile,as a common compound, the synthetic route is as follows.

6-(2-(Piperazin- 1 -yl)pyrimidin-5-yl)nicotinamide dihydrochloride (400 mg, 1.12 mmol), 3-(4-chlorobutyl)-1H-indole-5-nitrile (312 mg, 1.34 mmol), anhydrous sodium carbonate (712 mg, 6.72 mmol) and sodium iodide (50 mg, 0.33 mmol) were added into anhydrous acetonitrile (15 mL) in turn. The solution was heated to 90 C and reacted for 36 hours. The reaction was stopped, and the mixture was cooled to room temperature. The solvent was evaporated under reduced pressure. The residue was purified by column chromatography (dichloromethane/methanol (v/v) = 20/1) to give the title compound as a faint yellow solid (465 mg, 86.4%).MS (ESI, pos. ion) m/z: 481.30 [M+H].?H NIVIR (400 1?IFlz, DMSO-d6) (ppm): 11.36 (s, 1H), 9.08 (s, 2H), 9.04 (d, J= 1.7 Hz,1H), 8.26 (dd, J= 8.3, 2.1 Hz, 1H), 8.14 (s, 1H), 8.10 (s, 1H), 8.05 (d, J= 8.3 Hz, 1H), 7.52 (s,1H), 7.49 (d, J= 8.3 Hz, 1H), 7.40 (dd, J= 8.4, 0.9 Hz, 1H), 7.35 (s, 1H), 3.90 (brs, 4H), 3.39(brs, 4H), 2.73 (t, J 7.4 Hz, 2H), 2.452.39 (m, 2H), 1.731.65 (m, 2H), 1.54 (d, J= 6.7 Hz,2H);HPLC: 95.11%.

143612-79-7, 143612-79-7 3-(4-Chlorobutyl)-1H-indole-5-carbonitrile 9881123, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; JIN, Chuanfei; ZHONG, Wenhe; LIANG, Haiping; ZHANG, Yingjun; (79 pag.)WO2019/62662; (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

526-47-6, 5-Fluoro-2,3-dimethyl-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

526-47-6, General procedure: To a stirred (0.5 M) solution of indole or substituted indole (1 equiv.) in THF was added Boc2O (1.5 equiv.) and DMAP (0.1 equiv) at room temperature, and the mixture was stirred for 3 h. The reaction mixture was quenched with a saturated solution of NaHCO3 (20 mL) and extracted with EtOAc three times, and the combined organic layer was washed with brine and dried with Na2SO4. After removal of the solvent under reduced pressure, the residue was purified by column chromatography to give correspondent products.

As the paragraph descriping shows that 526-47-6 is playing an increasingly important role.

Reference£º
Article; Wu, Kui; Fang, Cheng; Kaur, Sarbjeet; Liu, Peng; Wang, Ting; Synthesis; vol. 50; 15; (2018); p. 2897 – 2907;,
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

81224-16-0, 7-Bromo-4-methoxy-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

81224-16-0, An oven-dried screw cap test tube was charged with a magnetic stir bar, CuCN (152.4 mg, 0.8mmol), then 34 (6.8 g, Y = 70.1%) in DMF (75 mL) was added into the tube. The reaction mixture wasstirred at 140 C overnight. After cooled down to room temperature, the resulting solution wasfiltered through Celite. The filtrate was diluted with ethyl acetate (100 mL) and washed withsaturated NaHCO3 solution (30 mL), water (30 mL) and brine (30 mL). The organic phase was driedover anhydrous Na2SO4, filtered and concentrated under reduced pressure. The residue was purifiedby silica gel column (petroleum ether/ethyl acetate = 1:1, v/v) to give 35 as a yellow solid (3.4 g, yield %). LC-MS (ESI): m/z [M + 1]+ = 173.10.

81224-16-0 7-Bromo-4-methoxy-1H-indole 3695499, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Meuser, Megan E.; Rashad, Adel A.; Ozorowski, Gabriel; Dick, Alexej; Ward, Andrew B.; Cocklin, Simon; Molecules; vol. 24; 8; (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