Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1477-50-5,1H-Indole-2-carboxylic acid,as a common compound, the synthetic route is as follows.

Under N2, to a solution of indole-2-formic acid (1.93g, 12mmol) in 120mL of dry Et2O was added19mL of MeLi solution dropwise (1.3M in Et2O, 24mmol) at 0C. The mixture was heated to reflux andkept for 2h and then cooled to room temperature. The saturated NH4Cl solution was added carefully to quench the reaction. The aqueous phase was extracted with Et2O and the combined organic phase waswashed with brine, dried with anhydrous MgSO4 and evaporated in vacuo. The crude product was purified by flash chromatography (PE : EA = 7 : 1) to give a white solid in 53% yield.

1477-50-5, The synthetic route of 1477-50-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Wu, Zhijie; Li, Ying; Cai, Yu; Yuan, Junying; Yuan, Chengye; Bioorganic and Medicinal Chemistry Letters; vol. 23; 17; (2013); p. 4903 – 4906;,
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

16502-01-5, 2,3,4,9-Tetrahydro-1H-pyrido[3,4-b]indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(B) will be 516 mg intermediate A dissolved in CH2Cl2In, adding 443 mg of benzoyl chloride (BzCl), under the condition in the ice bath, slowly dropping 455 mg triethylamine (Et3N), stirring at room temperature the reaction 2 h, monitoring after the reaction is complete, the reaction system for CH2Cl2(20 ml) dilution, then adding pure water extraction three times, and finally a saturated salt water, extracted into the organic phase collected drying, turns on lathe does, over silica gel column chromatography separation to obtain 671 mg of intermediate B2, column chromatography in eluting agent is PE/EtOAc=2:1, the reaction yield is 81%; product is a white solid at room temperature.

16502-01-5, 16502-01-5 2,3,4,9-Tetrahydro-1H-pyrido[3,4-b]indole 107838, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Fuzhou University; Chen Haijun; Ye Jinxiang; Wu Jianlei; Lv Tingting; Li Cailong; Gao Yu; (13 pag.)CN106883230; (2017); 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.22246-66-8,5-Methoxyisoindolin-1-one,as a common compound, the synthetic route is as follows.

Under an atmosphere of nitrogen, an ice-cooled solution of 6-methoxyisoindolin-1-one (commercially available from for example Astatech) (105 mg, 0.64 mmol) in DMF (2.5 mL) was treated with sodium hydride (60% w/w in mineral oil) (31 mg, 0.77 mmol) and the mixture was allowed to warm to ambient temperature. The mixture was then treated with ethyl 2-bromo-3-methylbutanoate (commercially available from for example Alfa Aesar) (135 mg, 0.64 mmol) and the mixture was stirred for 18 hours then cautiously treated with saturated aqueous ammonium chloride (20 mL). The product was extracted with ethyl acetate (2*25 mL) and the combined organic phase was washed with water (20 mL), brine (20 mL), filtered through a hydrophobic fit and evaporated to dryness. the product was purified by flash chromatography (20 g silica cartridge) using a gradient elution from 0 to 50% ethyl acetate in cyclohexane to afford the title compound (40 mg, 21% yield). LCMS RT=1.03 min, ES+ve m/z 292 [M+H]+

22246-66-8, 22246-66-8 5-Methoxyisoindolin-1-one 22064719, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Crews, Craig M.; Buckley, Dennis; Ciulli, Alessio; Jorgensen, William; Gareiss, Peter C.; Van Molle, Inge; Gustafson, Jeffrey; Tae, Hyun-Seop; Michel, Julien; Hoyer, Dentin Wade; Roth, Anke G.; Harling, John David; Smith, Ian Edward David; Miah, Afjal Hussain; Campos, Sebastien Andre; Le, Joelle; US2014/356322; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.50820-65-0,Methyl 1H-indole-6-carboxylate,as a common compound, the synthetic route is as follows.

50820-65-0, To a solution of methyl 1H-indole-6-carboxylate (124 g, 708 mmol) in tetrahydrofuran (500 ml) was added 4-dimethylaminopyridine (865 mg, 7 mmol). Then, a solution of di-tert-butyl dicarbonate (156 g, 715 mmol) in tetrahydrofuran (150 ml) was added dropwise at room temperature over about 1 hr, and the mixture was stirred for 1 hr. The reaction mixture was concentrated, and the residue was purified by silica gel chromatography to give the title compound (193 g, yield 99percent).1H-NMR (400 MHz, DMSO-d6) delta: 1.65 (9H, s), 3.89 (3H, s), 6.82H, dd, J=3.63, 0.86 Hz), 7.74 (1H, d, J=8.06 Hz), 7.85 (1H, dd, J=8.06, 0.86 Hz), 7.87 (1H, d, J=3.63 Hz), 8.76 (1H, d, J=0.81 Hz).

50820-65-0 Methyl 1H-indole-6-carboxylate 639844, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; JAPAN TOBACCO INC.; US2011/306599; (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

32387-21-6, 1-Methyl-1H-indole-3-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0132] Example 9: Synthesis of N-{[3′-bromo-4′-(1H-tetraazol-5-ylmethoxy)-1,1′- BIPHENYL-4-YL] METHYL}-N, L-DIMETHYL-LH-INDOLE-3-CARBOXAMIDE.; [0133] Step 1: 1-METHYL-LH-INDOLE-3-CARBONYL chloride. Oxalyl chloride (7.1 mL, 81.4 mmol) in 50 ML of methylene chloride was added under nitrogen dropwise to a solution of 1-methyl-1H-indole carboxylic acid (2. 86G, 16.3 mmol) in 100 mL of methylene chloride at room temperature. After the addition the reaction was stirred at room temperature until the reaction was determined by NMR analysis to be complete. The solvent and excess oxalyl chloride were removed under reduced pressure. The residue was taken up in benzene and then concentrated to dryness under reduced pressure to give l-methyl-lH-indole-3-carbonyl chloride, which was used in the following reaction without purification.

32387-21-6, As the paragraph descriping shows that 32387-21-6 is playing an increasingly important role.

Reference£º
Patent; WYETH; WO2005/30702; (2005); 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

32387-21-6, 1-Methyl-1H-indole-3-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Compounds 9e-35e were obtained by using one-pot reaction. A mixture of aromatic acid (6.30 mmol), EDCI (7.50 mmol), DMAP (0.60 mmol), and anhydrous dichloromethane (20 mL) was stirred to dissolve, then decane-diamine (3 mmol) was added and stirred at room temperature for 12 h. The mixture solution was filtered under reduced pressure. After that, the residue was washed with little amount of CH2Cl2and water successively, and dried to give the solid. Then, the residue was purified on preparative TLC eluted with chloroform/methanol = 40:1-7:1 to yield compounds 26e, 28e, 30e, and 31e., 32387-21-6

As the paragraph descriping shows that 32387-21-6 is playing an increasingly important role.

Reference£º
Article; Wang, Jiawen; Hong, Ge; Li, Guoliang; Wang, Wenzhi; Liu, Tianjun; Molecules; vol. 24; 24; (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

387-43-9, 4-Fluoroindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-fluoro-1H-indole (1.0 g, 7.400 mmol) and TFA (5.667 mL, 74.00 mmol) in CH2C12(25 mL) was added triethylsilane (3.546 mL, 22.20 mmol). The reaction was stirred at 23 ¡ãC for 15 h before quenched with saturated NaHC03. The mixture was extracted with DCM. The organic extract was concentrated. The residue was purified by preparative HPLC to give the title compound (0.15 g). LCMS m/z = 137.8 [M+H]+., 387-43-9

As the paragraph descriping shows that 387-43-9 is playing an increasingly important role.

Reference£º
Patent; ARENA PHARMACEUTICALS, INC.; SEMPLE, Graeme; BEHAN, Dominic P.; FEICHTINGER, Konrad; GLICKLICH, Alan; GROTTICK, Andrew J.; KAM, Maria Matilde Sanchez; KASEM, Michelle; LEHMANN, Juerg; REN, Albert S.; SCHRADER, Thomas O.; SHANAHAN, William R.; WONG, Amy Siu-Ting; ZHU, Xiuwen; WO2015/66344; (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

95-20-5,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.95-20-5,2-Methylindole,as a common compound, the synthetic route is as follows.

To a solution of 2-methylindole (10.04 g, 75 mmol) in toluene (200 mL) are added 2-chloroethylamine hydrochloride (17.4 g, 150 mmol), freshly powdered NaOH (21.00 g, 525 mmol) and tetrabutyl ammonium hydrogen sulfate (2.037 g, 6 mmol). The resulting mixture is heated up to reflux and stirred for 17h. It is then cooled down to RT, and filtered through a filter paper. The residue is triturated twice with toluene, and filtrated. The filtrate is concentrated under reduced pressure, and the residue is purified by FC, using a gradient of DCM/MeOH from 100:0 to 95:5. After concentration of the product containing fractions, the title compound (13.2 g, 99%) is obtained as a yellow resin: LC-MS A: tR = 0.54 min; [M+H]+ = 175.31.

The synthetic route of 95-20-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ACTELION PHARMACEUTICALS LTD; FRETZ, Heinz; LYOTHIER, Isabelle; POTHIER, Julien; RICHARD-BILDSTEIN, Sylvia; SIFFERLEN, Thierry; WYDER PETERS, Lorenza; POZZI, Davide; CORMINBOEUF, Olivier; (306 pag.)WO2017/85198; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.184150-96-7,Methyl 2-methyl-1H-indole-6-carboxylate,as a common compound, the synthetic route is as follows.

EXAMPLE 29 Production of 3-(2,4-dichlorobenzyl)-6-(methoxycarbonyl)-2-methylindole (58) 6-(Methoxycarbonyl)-2-methylindole (3.03 g), 2,4-dichlorobenzyl chloride (4.69 g) and silver(I) oxide (5.56 g) are suspended in 1,4-dioxane (50 ml), and stirred under heat at 90 C. for 19.5 hours. The solid is separated through filtration, and the filtrate is concentrated. The resulting residue is purified through silica gel column chromatography to obtain 3-(2,4-dichlorobenzyl)-6-(methoxycarbonyl)-2-methylindole (58) (1.15 g). 1H-NMR (CDCl3, delta ppm): 2.40 (3H, s), 3.92 (3H, s), 4.10 (2H, s), 6.84 (1H, d, J=8.3 Hz), 7.04 (1H, dd, J=2.1 and 8.4Hz), 7.31 (1H, d, J=8.3 Hz), 7.40 (1H, d, J=2.1 Hz), 7.73 (1H, dd, J=1.4 and 8.3 Hz), 8.06 (1H, d, J=1.1 Hz), 8.14 (1H, brs).

184150-96-7, The synthetic route of 184150-96-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Cell Pathways, Inc.; US6410584; (2002); 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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.15861-24-2,Indole-5-carbonitrile,as a common compound, the synthetic route is as follows.

General procedure: The procedure for the synthesis of the tetrazole 2a is representative. A mixture of sodium azide (0.39 g 0.0060 mol), urea (0.36 g, 0.0060 mol) and water (2.5 mL) was taken in a round-bottom flask and stirred at 60 C for 1 h. Charged benzonitrile 1a (0.5 g 0.0048 mol), acetic acid(0.5 mL) and DMF (2.5mL) at 60 C and heat to 110C stirred for 8 h. After completion of the reaction (as indicated by TLC), the reaction mixture was cooled to room temperature and diluted the reaction mass with water (2.5 mL)and ethyl acetate (5.0 mL) at 25-35 C. Add 5N aqueous hydrochloric acid (2.5 mL) at 25-35 C. Stirred for 20- 30 min, the resultant organic layer was separated and the aqueous layer was extracted with ethyl acetate (2.5 mL). The combined organic layer was washed with 40 % aq.NaCl solution (2.5 mL) and dried over anhydrous Na2SO4 and concentrated to give a crude product, which was isolated using chilled water after 3-4 h maintenance, and eventually filtered off to give 0.67 g (95%) of an off-white solid., 15861-24-2

The synthetic route of 15861-24-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Yakambram; Jaya Shree; Srinivasula Reddy; Satyanarayana; Naveen; Bandichhor, Rakeshwar; Tetrahedron Letters; vol. 59; 5; (2018); p. 445 – 449;,
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