Tag: M.W:100-200

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, A mixture of methyl lH-indole-6- carboxylate (1.75 g, 10 mmol) and NaH (0.52 g, 13 mmol, 60percent in oil) in THF (20 mL) was stirred at r.t. for 30 min, followed by addition of a solution of 4-methylbenzene-l-sulfonyl chloride (2.85 g, 15 mmol) in THF (5 mL). The reaction mixture was stirred at r.t. for another lhr, then quenched with water and extracted with EtOAc. The combined organic layers were dried over anhydrous Na2SC>4 and concentrated under reduced pressure. The residue was purified by column chromatography to give the desired product (2.8 g, 85percent yield).LCMS: m/z 330 (M+H)+.

As the paragraph descriping shows that 50820-65-0 is playing an increasingly important role.

Reference£º
Patent; SPERO THERAPEUTICS, INC.; ZAHLER, Robert; (262 pag.)WO2016/112088; (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.91-55-4,2,3-Dimethyl-1H-indole,as a common compound, the synthetic route is as follows.

General procedure: In a flame dried flask the imidate (1.0 equiv) was dissolved in anhydrous 1,2-dichloroethane(0.15 M) followed by the addition of the indole (1.5 equiv). To this solution freshly distilledTMSOTf (0.2 equiv) was added and the resulting mixture was stirred at rt for 3 h. The reactionmixture was then quenched with the addition of 1M NaOH. The organic layer was separated andthe aqueous layer was extracted with DCM (2x). The combined organic extracts were dried oversodium sulfate, filtered and concentrated. The residue was then purified by silica gelchromatography using the solvent systems listed for each compound., 91-55-4

The synthetic route of 91-55-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Adhikari, Arijit A.; Radal, Lea; Chisholm, John D.; Synlett; vol. 28; 17; (2017); p. 2335 – 2339;,
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.830-96-6,3-Indolepropionic acid,as a common compound, the synthetic route is as follows.

To a solution of 3-(lH-indol-3-yl)propanoic acid (1.5 g, 7.9 mmol) in THF (20 mL) was added 1M BH3 in THF (9 mL, 9 mmol) at 0 C. The reaction mixture was stirred for 1 h at 0 C and quenched by addition of MeOH then concentrated in vacuo. The residue was purified by flash chromatography (Combi-flash Rf Hexane/EtOAc gradient 0-25%) to give the title compound as a white solid in 1.2 g (7.1 mmol). MS (ES) 176.1 (M+H)., 830-96-6

830-96-6 3-Indolepropionic acid 3744, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; VANDERBILT UNIVERSITY; LEE, Taekyu; BIAN, Zhiguo; BELMAR, Johannes; CHRISTOV, Plamen P.; PELZ, Nicholas F.; SHAW, Subrata; KIM, Kwangho; TARR, James C.; OLEJNICZAK, Edward T.; ZHAO, Bin; FESIK, Stephen W.; WO2015/148854; (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

4769-97-5,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4769-97-5,4-Nitroindole,as a common compound, the synthetic route is as follows.

General procedure: In a typical reaction, DAC (0.20 mmol) was mixed with indole (0.20 mmol) and PTSA (10 molpercent) in ethanol (1.0 mL). The mixture was then stirred at 60¡ãC for 20 min. After reaction, the mixture was cooled to room temperature, and the product was obtained by isolation with preparative TLC (eluting solution: petroleum ether/ethyl acetate=5/1 (v/v)). Tests for substrate scope were all performed with an analogous procedure. Large scale synthesis was also performed in a similar procedure. The product was isolated by silica column chromatography (eluting solution: petroleum ether/ethyl acetate=8/1 (v/v)).

4769-97-5 4-Nitroindole 145766, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Liu, Changhui; Zhou, Li; Huang, Wenbo; Wang, Man; Gu, Yanlong; Tetrahedron; vol. 72; 4; (2016); p. 563 – 570;,
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

5416-80-8, 2-Methyl-1H-indole-3-carbaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2-Methyl-indole-3-carbaldehyde (1) (2.1?g, 10.0mmoles) in Benzene (50?mL) containing 50% NaOH solution (25?mL), tetrabutylammonium hydrogensulfate (100?mg) and P-Toluenesulfonyl chloride (1.31?g, 10.0mmoles) were added. The mixture was stirred well for 4?h. hen it was poured over crushed ice and extracted with ethyl acetate (3?*?50?mL). The organic layer was separated, washed with water (3?*?25?mL) and dried (MgSO4). Crystallization process by slow solvent evaporation technique using ethyl acetate gave the desired product in 87% yield., 5416-80-8

As the paragraph descriping shows that 5416-80-8 is playing an increasingly important role.

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Article; Bellamkonda, Yagna Narayana; Vijaya Chamundeeswari; Journal of Molecular Structure; vol. 1181; (2019); p. 613 – 626;,
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.399-72-4,5-Fluoro-2-methylindole,as a common compound, the synthetic route is as follows.

Example 1; 2-Pyridin-3-yl-pyrimidine-5-carboxylic acid (5-fluoro-2-methyl-indol- 1 -yl)-amide; Step 1 : A solution of potassium tert-butoxidc (1.84 g, 16.43 mmol) and 5-fluoro-2- methylindole (1.21 g, 8.09 mmol) in DMF (20 mL) is stirred under N2 at rt for 60 min. A solution of monochloroamine in ether (65 mL, 9.75 mmol) is added via an addition funnel over 10 min. The resulting mixture is stirred at 23C for 2 hours, and then concentrated in vacuo. The residue is partitioned between EtOAc and water. The organic phase is separated, washed with saturated aqueous NaHCO3, water and brine, dried (MgSO4), filtered and concentrated in vacuo. The residue is purified by silica gel chromatography eluting with 10% EtOAc in heptane to afford 5 -fluoro-2-methyl-indol- 1 -ylamine (290 mg, 22%) as a solid. MS: 165 (M+H); 1H NMR (300MHz, CDCl3): delta 7.24-7.19 (m, IH), 7.12 (dd, IH), 6.92 (dt, IH), 6.12 (s, IH), 4.23 (br s, 2 H), 2.39 (s, 3H).

399-72-4, 399-72-4 5-Fluoro-2-methylindole 2778715, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
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

52415-29-9, 6-Bromoindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

52415-29-9, (a) 6-Bromo-1-methylindole STR25 Sodium hydride (4.10 g of a 60% dispersion in paraffin wax) was added to a stirred solution of 6-bromoindole (10 g, 51.3 mmol) in tetrahydrofuran (10 ml) at 0 C. under a nitrogen atmosphere. After 1 hour iodomethane (6.38 ml, 102.6 mmol) was added and the cooling bath removed. After 12 hours methanol was added dropwise until effervescence ceased and then the solvent was removed in vacuo. The thick residue was diluted with dichloromethane and washed first with water then with brine. The organic layer was dried (magnesium sulphate) and concentrated in vacuo to give a dark yellow oil. Filtration through a plug of silica with 90% hexane/10% ethyl acetate as eluant gave the subtitle compound as a pale yellow oil (10.5 g). 1 H NMR (300 MHz, CDCl3): delta=3.75 (d, 3 H), 6.40 (d, 1 H), 7.00 (d, 1 H), 7.20 (d, 1 H), 7.50 (d, 1 H), 7.45 (s, 1 H). LRMS (Thermospray): 209.7 (MH+)

As the paragraph descriping shows that 52415-29-9 is playing an increasingly important role.

Reference£º
Patent; Pfizer Inc.; US6017945; (2000); 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.1196-70-9,1H-Indole-6-carbaldehyde,as a common compound, the synthetic route is as follows.

1196-70-9, Step 3. Synthesis of (E)-N?-(( 1 H-indol-6-yl)methylene)-2-(2-(furan-3 -yl)-6- methylphenoxy)acetohydrazide: 2-(2-(furan-3 -yl)-6-methylphenoxy)acetohydrazide (70 mg,0.28 mmol) and 1H-indol-6-carbaldehyde (45 mg, 0.31 mmol) were dissolved in EtOH 2 mL, followed by stirring at 100 C for 12 hours. After the completion of the reaction, the reaction mixture was added with water, and extracted with ethyl acetate. The obtained organic layer was dried over magnesium sulfate, and purified by column chromatography (ethyl acetate:hexane = 1:1) to obtain Compound 313 (20 mg, 19%).?H NMR (400 MHz, DMSO-d6): 6 11.41 (m, 2H), 8.45-8.01 (2s, IH), 8.30 (m, IH), 7.72 (m,1H), 7.46 (m, 4H), 7.10 (m, 4H), 6.44 (m, 1H), 4.70 (s, 1H), 4.25 (s, 1H), 2.30 (m, 3H).

1196-70-9 1H-Indole-6-carbaldehyde 2773435, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; INJE UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION; CHOI, HoJin; LEE, JaeWon; LEE, ChangGon; HA, NiNa; SEO, Su Kil; LEE, SunMi; LEE, Song-Min; WO2014/35149; (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.1953-54-4,5-Hydroxyindole,as a common compound, the synthetic route is as follows.

A mixture ofof5-hydroxyindole 1 (750 mg, 5.63 mmol), benzyl bromide (1.05 g, 6.19 mmol), K2C03 (2.30 g, 16.89 mmol) and DMF (10 mL), was stirred at RT for 16 h. The mixture was partitioned between water (100 mL) and EtOAc (50 mL). The organic layer was separated and the aq. layer re-extracted with additional EtOAc (50 mL). The combined organic layers were dried over Na2SO4, filtered, and the filtrate concentrated under reduced pressure. The residue was purified (silica gel; eluting with 0-100% EtOAc in hexanes), to afford compound 2 (1.12 g, 88%) as a light yellow solid. LCMS Mass: 224.0 (M+1)., 1953-54-4

As the paragraph descriping shows that 1953-54-4 is playing an increasingly important role.

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Patent; PHARMAKEA, INC.; ROWBOTTOM, Martin, W.; HUTCHINSON, John, Howard; (185 pag.)WO2017/3862; (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.3189-22-8,7-Methoxyindole,as a common compound, the synthetic route is as follows.

7-methoxyindole (0.2 mmol) was added to a 4 mL reaction flask.1,2-diphenyldisulfide (0.3 mmol),Potassium tert-butoxide (0.4 mmol) and DMF (2.0 mL) were stirred at room temperature. TLC tracks the detection reaction. After 2 hours, the starting material was completely converted.Water and dichloromethane were added to the reaction system, and the organic layer was separated.Wash the water layer twice with dichloromethane, combine all the organic layers, andWash twice with water. The organic layer was dried over anhydrous sodium sulfate, concentrated, and then purified by column chromatography (To the product 32 mg, the yield was 63percent, and the reaction process was as follows:, 3189-22-8

3189-22-8 7-Methoxyindole 76660, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Wenzhou Medical University; Song Zengqiang; Zhan Lingling; Qian Jianchang; Liang Guang; Liu Zhiguo; (14 pag.)CN108586311; (2018); 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