Tag: M.W:100-200

22246-66-8, 5-Methoxyisoindolin-1-one is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,22246-66-8

To a suspension of (74) (7.07 g, 43.4 mmol) in CH2Cl2 (600 ml) was added BBr3(IM in CH2Cl2, 86.7 ml). The reaction mixture was stirred at room temperature for 4 hr. The solvent and boron residue was removed in vacuo and the remaining solid was dissolved in CH2Cl2, the solution was neutralized with 1 N NaOH (PH = 6.5). Desired compound was precipitated out and filtered. The organic solution was separated and washed with sat. NaCl, dried over Na2SO4 to give the title compound (combined weight 5.1 g, 78 %). MS (ES) m/z 150.1.

The synthetic route of 22246-66-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; WYETH; WO2006/138549; (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

830-96-6, 3-Indolepropionic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: H2SO4 (98%) (0.5mL) was added to a stirred solution of raw material1 in CH3OH (10mL) at room temperature and the mixture was then stirred for 2-3 h at 80 C. TLC was used to monitor the reaction progress until it was complete. A large amount of ice water was then added to the mixture. A saturated solution of sodium carbonate was used to neutralise the mixture until white solid appeared. After filtering the mixed solution, compounds 2a-h (yield 91-99) were obtained., 830-96-6

The synthetic route of 830-96-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Ye, Ying; Suo, Yourui; Yang, Fang; Yang, Yongjing; Han, Lijuan; Journal of Chemical Research; vol. 39; 5; (2015); p. 296 – 299;,
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.272-49-1,4-Azaindole,as a common compound, the synthetic route is as follows.

the mixture of the cyclic imine 3,4-dihydroisoquinoline (66 mg, 0.50 mmol);6,7-dihydrothieno[3,2-c]pyridine (51 mg, 0.38 mmol); 3,4-dihydro–carboline (63 mg, 0.38 mmol) or4,5-dihydro-3H-benz[c]azepine (55.3 mg, 0.38 mmol); and the electron-rich aromatic compound (7-, 6-,4-, or 5-azaindole (30 mg, 0.25 mmol)) were placed in a 10 mL pressurized reaction vial and heated ina microwave reactor, under the conditions given in Tables 1-3. In the case of 5-azaindole, 10 mol % ofp-TSA (4.3 mg, 0.025 mmol) as a catalyst was also added., 272-49-1

272-49-1 4-Azaindole 9226, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Belasri, Khadija; Fueloep, Ferenc; Szatmari, Istvan; Molecules; vol. 24; 19; (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

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

General procedure: To a suspension of 2-methylindole-3-carboxaldehyde (7a) (200 mg, 1.26 mmol) and Cs2CO3 (1.34 g, 3.80 mmol) in N,N-dimethylformamide (4 mL) was added 2-fluorobenzaldehyde (210 muL, 1.99 mmol) under a nitrogen atmosphere. The reaction mixture was heated at 140 C until the indole substrate was all consumed (monitored by TLC), and then allowed to cool down to room temperature. The resulting mixture was filtered and washed with ethyl acetate (80 mL). The filtrate was washed with water (3 X 80 mL). The organic layer was dried over Na2SO4 and concentrated under reduced pressure. The residue was purified by flash column chromatography on silica gel (EtOAc/hexanes = 1:3) to afford the desired indolo[1,2-a]quinoline.

5416-80-8, The synthetic route of 5416-80-8 has been constantly updated, and we look forward to future research findings.

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Article; Thanetchaiyakup, Adisak; Rattanarat, Hassayaporn; Chuanopparat, Nutthawat; Ngernmeesri, Paiboon; Tetrahedron Letters; vol. 59; 11; (2018); p. 1014 – 1018;,
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.1477-49-2,3-Indoleglyoxylic Acid,as a common compound, the synthetic route is as follows.

1477-49-2, General procedure: To a solution of carboxylic acid (2.05 equiv.), diamine (1 equiv.), and PyBOP (2.05 equiv.) in DMF (1 mL) was added Et3N (3 equiv.). The reaction mixture was allowed to stir under N2 at room temperature for 23 h. The solution was dried in vacuo and the crude reaction product purified by C8 reversed-phase column chromatography (20%-30% MeOH/H2O (+0.05%TFA)) to afford the target diamide as the bis-trifluoroacetate salt or by silica gel column chromatography (0%-1% MeOH in CH2Cl2) to afford the target diamide as the free base.

The synthetic route of 1477-49-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Wang, Jiayi; Kaiser, Marcel; Copp, Brent R.; Marine Drugs; vol. 12; 6; (2014); p. 3138 – 3160;,
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.35320-67-3,2-Methyl-1H-indol-4-ol,as a common compound, the synthetic route is as follows.,35320-67-3

To a stirred solution of 2-chloro-N-[(3- fluorophenyl)methyl]-6,7-dihydro-5H-pyrano[2,3-d]pyrimidin-4-amine (7 g, 23.83 mmol) in anhydrous dioxane (140 mL) were added 2-methyl-1H-indol-4- ol (3.5 g, 23.83 mmol), Pd2dba3 (2.9 g, 2.38 mmol), X-Phos (2.3 g, 4.77 mmol) and Cs2CO3 (15.5 g, 47.66 mmol). The suspension was refluxed under N2 for 2 h. LCMS showed the reaction was completed. The mixture was filtered through a pad of celite, and the filter cake was washed with EtOAc (200 mL x 2). The organics were combined and concentrated in vacuo. The red residue was solidified by MTBE and EtOAc (100 mL/20 mL), the solid was collected by filtration and dried in vacuo to afford the product (7.5 g, 77%) as a brown solid. The filtrate was concentrated in vacuo and purified by silica gel column (hexane and ethyl acetate) to afford the 2nd fraction product (1.5 g) as a brown solid. LCMS (M+H+) m/z: Calcd: 405.1; Found: 405.1.

35320-67-3 2-Methyl-1H-indol-4-ol 590225, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; CLEAVE BIOSCIENCES, INC.; ZHOU, Han-Jie; WUSTROW, David; (498 pag.)WO2016/200840; (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

4264-35-1, 1-(1H-Indol-2-yl)ethanone is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,4264-35-1

5-Chloro-2-hydroxy-N’-((1E)-1-(1H-indol-2-yl)ethylidene)benzohydrazide (6t) To a mixture of methyl 5-chloro-2-hydroxybenzoate (162 mg, 0.87 mmol) in isobutanol (0.5 mL) was added hydrazine hydrate (42 muL, 0.87 mmol). The reaction mixture was irradiated with microwaves for 15 min at 115 C. Isobutanol was added and the supernatant was removed. The residue was taken up in isobutanol (0.5 mL) and 1-(1H-indol-2-yl)ethanone 3p (138 mg, 0.87 mmol) was added. The reaction mixture was again irradiated with microwaves for 10 min at 110 C. The solid product was filtered and then, triturated with EtOH and Et2O to afford 6t as a yellow solid (90 mg, 33%). Mp = 198-200 C. 1H NMR (400 MHz, DMSO-d6): delta 12.46 (s, 1H), 11.39 (s, 1H), 10.07 (s, 1H), 7.86 (d, J = 2.4 Hz, 1H), 7.60 (d, J = 7.6 Hz, 1H), 7.47 (d, J = 7.6 Hz, 1H), 7.41 (dd, J = 8.8 Hz, 2.4 Hz, 1H), 7.19 (tm, J = 7.6 Hz), 7.03 (m, 2H), 6.93 (d, J = 8.8 Hz, 1H), 2.48 (s, 3H). 13C NMR (100 MHz, DMSO-d6): delta 158.0, 153.8, 137.5, 136.5, 132.8, 127.7, 126.8, 123.4, 122.3, 120.9, 119.3, 119.1, 111.8, 104.9, 14.5. HRMS calcd for (C17H1435ClN3O2+Na)+ 350.0663, found 350.0667.

4264-35-1 1-(1H-Indol-2-yl)ethanone 589081, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Kumar, Nag S.; Amandoron, Emily A.; Cherkasov, Artem; Brett Finlay; Gong, Huansheng; Jackson, Linda; Kaur, Sukhbir; Lian, Tian; Moreau, Anne; Labriere, Christophe; Reiner, Neil E.; See, Raymond H.; Strynadka, Natalie C.; Thorson, Lisa; Wong, Edwin W.Y.; Worrall, Liam; Zoraghi, Roya; Young, Robert N.; Bioorganic and Medicinal Chemistry; vol. 20; 24; (2012); p. 7069 – 7082;,
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

348640-06-2, 4-Bromo-7-azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

As shown in Scheme 6,4-bromo-1H-pyrrolo[2,3-b]pyridine (1.01 g), 2-acetamidophenylboronic acid (1.63 g), Pd(PPh3)4 (0.345 mg), and 1M Na2CO3 (8 mL) were mixed in DME (20 mL) and heated at 95 C. overnight. The reaction was cooled and water (60 mL) added. Extraction with dichloromethane (3¡Á) and concentration of the combined organic extracts gave N-(2-(1H-pyrrolo[2,3-b]pyridin-4-yl)phenyl)acetamide (compound 1001), which was treated with concentrated hydrochloric acid (20 mL) and toluene (1 mL) and heated at 128 C. for 30 min. Evaporation of the volatiles gave a residue, to which saturated sodium bicarbonate was added. The resulting mixture was extracted with dichloromethane (3¡Á). Concentration of the organics and purification of the residue via silica gel chromatography (50 to 80% EtOAc/hexane) gave 2-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzenamine (compound 1002, 1.07 g). To compound 1002 (14 mg) in methanol (1 mL) was added 4N HCl-dioxane (0.05 mL) and benzaldehyde (16 mg). The reaction mixture was capped and heated at 90 C. for 1 h. About 75% of the methanol was removed by evaporation, followed by the addition of ethyl ether (5 mL). The resulting solid was filtered and washed with ether (2¡Á) to yield compound 5 as the hydrochloride salt (22.5 mg)., 348640-06-2

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

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Patent; Vertex Pharmaceuticals Incorporated; US2010/81645; (2010); 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.40913-43-7,1-Ethyl-1H-indole-2-carbaldehyde,as a common compound, the synthetic route is as follows.

Intermediate 2 l-Ethyl-3-fluoro-l//-indole-2-carbaldehydeA 50 mL round bottom flask was charged with 1 -ethyl- 1 H- indole-2-carbaldehyde (Intermediate 1, 524 mg, 3.03 mmol) and Selectfluor (1.29 g, 3.64 mmol). MeCN (6.0 mL) was added, and the mixture was allowed to stir at room temperature. After 90 min, the solvent was removed in vacuo, and the residue was partitioned between EtOAc and H2O, and the aqueous layer was further extracted with EtOAc. The combined organic layers were washed with brine, dried (MgSO4), filtered, and concentrated. The crude material was purified by silica gel chromatography (gradient elution; Rf in 95:5 hexanes:EtOAc = 0.42) to give a colorless solid (191 mg, 33%) of 90% purity (remainder is unreacted starting material). 1H NMR (400 MHz, CDCl3) delta 1.31 – 1.39 (m, 3 H) 4.52 (q, J=7.07 Hz, 2 H) 7.16 (m, 1 H) 7.34 (m, 1 H) 7.38 – 7.45 (m, 1 H) 7.70 (m, 1 H) 10.08 (s, 1 H). M/Z 191.

40913-43-7, As the paragraph descriping shows that 40913-43-7 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2008/59238; (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

271-34-1, 5-Azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of triethylamine (0.65 ml, 4.66 mmol) and 5-azaindole (1.00 g, 8.46 mmol) in MeCN (20 ml) stirring at 0 00 was added di-teit-butyl dicarbonate (0.97 ml,4.23 mmol) dropwise under nitrogen with stirring. The reaction was allowed to warm to room temperature and left to stir over the weekend. Further di-teit-butyl dicarbonate (0.97 ml, 4.23 mmol) was added and stirring continued for 6 hours. The reaction mixture was concentrated under reduced pressure and the oil obtained taken up in DCM and washed with water. The mixture was passed through a hydrophobic frit and solvent removed under reduced pressure to afford teit-butyl pyrrolo[3,2-c]pyridine-1-carboxylate (P62) (1.76 g), LCMS ES 219 [M+H], Rt = 1.19 mins (Generic Basic Method)., 271-34-1

The synthetic route of 271-34-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; PUGLIESE, Angelo; FRANCIS, Stuart; MCARTHUR, Duncan; SIME, Mairi; BOWER, Justin; BELSHAW, Simone; (315 pag.)WO2019/34890; (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