Day: November 4, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.166104-20-7,1-Boc-5-Aminoindole,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl 5-amino-1H-indole-1-carboxylate (1, 5.0 g, 21.55 mmol) in acetonitrile (50 mL) at 0 C., N-bromosuccinimide (4.23 g, 23.70 mmol) was added portion-wise. The mixture was stirred at same temperature for 3 h. Next, the reaction was poured into ice-cold water and extracted with ethyl acetate. The organic layer was washed with brine solution, dried over anhydrous sodium sulfate, filtered, and concentrated to dryness under reduced pressure. The crude product was purified by Combiflash (40 g, RediSep column) using 0-30% ethyl acetate in hexanes as eluent. The desired fractions were concentrated under reduced pressure to afford tert-butyl 5-amino-4-bromo-1H-indole-1-carboxylate (2) as a brown liquid. Yield: 5.8 g, 86%; MS (ESI) m/z 311.08 [M+1]+., 166104-20-7

166104-20-7 1-Boc-5-Aminoindole 11593831, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; eFFECTOR Therapeutics, Inc.; ERNST, Justin T.; REICH, Siegfried H.; SPRENGELER, Paul A.; XIANG, Alan X.; (41 pag.)US2019/119256; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.398487-76-8,4-Fluoro-2-methyl-1H-indol-5-amine,as a common compound, the synthetic route is as follows.

Step 12f: Ethyl 7-(7-(benzyloxy)-4-(4-fluoro-2-methyl-1H-indol-5-ylamino)quinazolin-6-yloxy)-heptanoate (compound 601-20) The title compound 601-20 (100 mg, 52%) was prepared as a dark solid from compound 507-20 (150 mg, 0.34 mmol) and 402 (67 mg, 0.41 mmol) using a procedure similar to that described for compound 601-18 (Example 10): LCMS: 571 [M+1]+; 1H NMR (DMSO-d6): delta 11.22 (s, 1H), 9.33 (s, 1H), 8.20 (s, 1H), 7.84 (s, 1H), 7.50 (d, J=8.4 Hz, 2H), 7.43-7.32 (m, 3H), 7.21 (s, 1H), 7.10 (d, J=8.4 Hz, 1H), 6.97 (t, J=8.4 Hz, 1H), 6.19 (s, 1H), 5.29 (s, 2H), 4.11 (t, J=8.7 Hz, 2H), 4.00 (q, J=6.00 Hz, 2H), 2.38 (s, 3H), 2.26 (t, J=7.5 Hz, 2H), 1.82-1.76 (m, 2H), 1.57-1.35 (m, 6H), 1.14 (t, J=7.5 Hz, 3H)., 398487-76-8

The synthetic route of 398487-76-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Qian, Changgeng; Cai, Xiong; Zhai, Haixiao; US2009/76044; (2009); 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.6960-42-5,7-Nitro-1H-indole,as a common compound, the synthetic route is as follows.,6960-42-5

General procedure: Phthaldialdehyde (1 mmol) was dissolved in glacial acetic acid (15 mL). Then, the corresponding indole (2 mmol) was added to the solution. The mixture was stirred under reflux conditions at 100 C until all of the starting phthaldialdehyde had disappeared, according to TLC-monitoring in CH2Cl2 (100%). The reaction time varied from 2 to 12 h. The reaction mixture was worked up by a dropwise neutralizing of the acid with NaOH (10%) until a pH of 7 was reached, followed extraction with CH2Cl2 (50 mL) for three times. The organic layer was washed with water and brine each for three times.Then it was dried over sodium sulphate, filtered and concentrated in vacuum. The reaction products were given after column chromatography using silica gel and ethyl acetate/cyclohexane mixtures as eluent. The resulting fractions (each 10 mL) were analyzed by TLC to identify the compound containing fractions which were unified and evaporated to dryness to give the target compounds. 11-(1H-Indol-3-yl)-5H-benzo[b]carbazole (3a).

6960-42-5 7-Nitro-1H-indole 23396, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Ashraf, Kerolos; Yasrebi, Kaveh; Hertlein, Tobias; Ohlsen, Knut; Lalk, Michael; Hilgeroth, Andreas; Molecules; vol. 22; 12; (2017);,
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.288385-88-6,4-Fluoro-5-hydroxy-2-methylindole,as a common compound, the synthetic route is as follows.

The above product was mixed with DMAP (1.5 eq), 2-methyl-4-fluoro-5-hydroxyindole (WO0047212) (1 eq) in dioxane (20 ml). The reaction was refluxed for three days and diluted with EtOAc, water and extracted with EtOAc three times. The combined organic layer was washed with water, brine and dried. The solution was evaporated and purified with silica gel column to give the titled product (300 mg). Mass: (M+1), 451

288385-88-6, The synthetic route of 288385-88-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Advenchen Laboratories, LLC; US2008/227811; (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

52562-50-2, 5-Methyl-1H-indole-3-carbaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

52562-50-2, General procedure: A mixture of 1 (20 mmol) and 2 (10 mmol) and water (5 ml) was refluxed at 100 C1 h. At the end of this period, an orange-colored solid was separated from the reaction mixture which was collected by filtration. The isolated solid was washed with hot water (10 ml 9 3), dried, and recrystallized from ethanol to obtain pure 4.

52562-50-2 5-Methyl-1H-indole-3-carbaldehyde 259187, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Madhu, Bandi; Raja sekar; Venkata Ramana Reddy; Dubey; Research on Chemical Intermediates; vol. 43; 12; (2017); p. 6993 – 7012;,
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

1670-83-3, Indole-7-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 23; Preparation of 1H-Indole-7-carboxylic acid (4-tert-butyl-benzyl)-phenethyl-amide; To a solution of 48 mg (0.3 mmol) of 1H-indole-7-carboxylic acid and 96 mg of TBTU (0.3 mmol) in 4 ml DMF, were added 0.26 ml (1.5 mmol) of N,N-diisopropylethyl amine. After stirring for 5 min at rt, 80 mg (0.3 mmol) of (4-tert-butyl-benzyl)-phenethyl-amine in 1 ml DMF were added. After stirring for 5 h at rt, the reaction mixture was diluted with 50 ml water and extracted with 2¡Á50 ml EtOAc. The combined organic phases were washed with water and brine, dried with magnesium sulfate, filtered and concentrated in vacuo. The residue was purified by column chromatography (8 g silica gel; EtOAc/heptane 1:6) to give 100 mg white solid (80%). MS (ISP) 411.5 (M+H)+.

1670-83-3, The synthetic route of 1670-83-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Conte-Mayweg, Aurelia; Kuehne, Holger; Luebbers, Thomas; Maugeais, Cyrille; Mueller, Werner; Pflieger, Philippe; US2006/30613; (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

15861-24-2, Indole-5-carbonitrile is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,15861-24-2

Compound 1 (142.2g, 1.0mol) was dissolved in dichloromethane (1.5L), the internal temperature was controlled at 0-5 C, and anhydrous zinc chloride (150g, 1.1mol) was added.After the addition was completed, the temperature was lowered to about -10 C, and 1-bromo-4-chlorobutane (Compound 3) (188.6g, 1.1mol) was added dropwise.After the dropwise addition was completed, the temperature was raised to a reaction temperature of 0 C and the reaction was conducted for 2 hours.After the reaction was completed, dichloromethane (0.5 L) was diluted, and ice water (1 L) was destroyed. Subsequently, 1 N sodium hydroxide solution was added to neutralize to adjust pH = 7, and extraction and liquid separation were performed.The organic phase was washed with saturated brine (0.5 L) and separated.After the organic phase was concentrated to dryness, the residue was recrystallized from isopropyl acetate (0.5 L),205 g of the product (I) was obtained, the yield was 88%, and the HPLC purity was 99.62%.

As the paragraph descriping shows that 15861-24-2 is playing an increasingly important role.

Reference£º
Patent; Shanghai Institute of Technology; Fang Yahui; Li Huixia; (6 pag.)CN111087340; (2020); 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

348-36-7, Ethyl 5-fluoro-1H-indole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

a) To a solution of 5-fluoroindol-2-ethyl ester (200 mg, 0.965 mmol) in dimethylsulfoxide (6 mL) is added potassium tert-butylate (108 mg, 0.965 mmol) and the mixture is stirred at 50¡ã C. for 30 minutes. After cooling to room temperature bromoethane (0.081 mL, 1.06 mmol) is added and the mixture is stirred at room temperature for 2.5 hours. With cooling water is added and the mixture is extracted with ethyl acetate. The organic layer is washed with water and saturated aqueous NaCl solution, dried over MgSO4 and the solvent is evaporated in vacuo to yield 200 mg of 1-ethyl-5-fluoro-1H-indole-2-carboxylic acid ethyl ether (ESI mass spectrum: [M+H]+=236).

348-36-7, As the paragraph descriping shows that 348-36-7 is playing an increasingly important role.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; Anderskewitz, Ralf; Martyres, Domnic; Oost, Thorsten; Rist, Wolfgang; Seither, Peter; US2013/23576; (2013); 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

103858-53-3, Ethyl 6-bromoindole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

103858-53-3, Example 1 6-(4-TERT-BUTYLPHENYL)-1-(3-PHENOXYBENZYL)-3-PHENYLINDOLE-2-CARBOXYLIC acid (a) 6-(4-tert-Butylphenyl)indole-2-carboxylic acid ethyl ester A mixture of 6-BROMOINDOLE-2-CARBOXYLIC acid ethyl ester (400 mg, 1.5 mmol), 4-TERT-BUTYLPHENYLBORONIC acid (400 mg, 2.25 mmol), K3P04 (950 mg, 1.5 mmol), Pd (OAC) 2 (18 mg, 0.075 mmol), 2,2′-bis (di-tert- BUTYLPHOSPHINO)-L, l’-biphenyl (45 mg, 0.15 mmol), and toluene (9 ML) were stirred in an argon atmosphere for 30 min at room temperature, and at 100 C for 40 min using microwave irradiation. The mixture was cooled to room temperature and poured into NaHCO3 (aq. , sat. ). The mixture was extracted with EtOAc and the combined extracts were washed with water, brine and dried over NA2S04. The organic phase was then concentrated and the product purified by chromatography to give the sub-title compound (392 mg, 81%).

As the paragraph descriping shows that 103858-53-3 is playing an increasingly important role.

Reference£º
Patent; BIOLIPOX AB; MCNEENEY, Stephen, Phillip; WO2005/5415; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.128562-95-8,4-(Trifluoromethyl)-1H-indole,as a common compound, the synthetic route is as follows.

A. 1 -(2-Methoxy-ethyl)-4-trifluoromethyl-1 H-indole A mixture of 4-trifluoromethyl-1 H-indole (105 mg, 0.57 mmol), powder KOH (159 mg, 2.83 mmol) in DMSO (6 mL) is stirred at r.t. for 5 min. 2-Methoxyethyl bromide (80 muIota_, 0.85 mmol) is added. After the reaction mixture is stirred at r.t. overnight, it is partitioned between H2O and Et2O. The two layers are separated, and the aqueous layer is extracted with Et2O (3x). The combined organic extracts are washed with H2O and brine, dried over MgSO , filtered, and concentrated in vacuo. The crude material is purified on silica gel with heptane/EtOAc (100/0 to 70/30) as eluent to yield the product (100 mg, 72%) as a clear colorless liquid.1 H NMR (300 MHz, CDCI3) delta 7.53 (d, J = 8.2 Hz, 1 H), 7.40 (d, J = 7.3 Hz, 1 H), 7.35- 7.20 (m, 2H), 6.69 (s, 1 H), 4.32 (t, J = 5.4 Hz, 2H), 3.71 (t, J = 5.4 Hz, 2H), 3.31 (s, 3H);19F NMR (300 MHz, CDCI3) delta -60.99 (s, 3F);LC Rt: 3.21 min; MS 244 (M+H, 100%)., 128562-95-8

128562-95-8 4-(Trifluoromethyl)-1H-indole 19803703, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; SANOFI; CHOI-SLEDESKI, Yong Mi; LIANG, Guyan; NIEDUZAK, Thaddeus R.; POLI, Gregory B.; SHUM, Patrick Wai-Kwok; STOKLOSA, Gregory T.; ZHAO, Zhicheng; WO2011/79102; (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