Tag: M.W:200-300

16732-64-2, 4-Bromo-1H-indole-2-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

a) 4- (2-Ethylphenyl)-indole-2-carboxylic acid; To a mixture of 0.28 g of 4-bromo-indole-2-carboxylic acid and 0.069 g of tetrakistriphenylphosphinepalladium in 11 ml of toluene and 2 ml of 2M soda is added a solution of 0.300 g of 2-ethylphenylboronic acid in 3 ml of ethanol. This mixture is refluxed for 16 h, filtered and the aqueous phase acidified with 2N HCI and extracted with ethyl acetate. Concentration of the organic phase gives the product as a brownish powder, m. p. 230-233, sufficiently pure for the next step.

16732-64-2, The synthetic route of 16732-64-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2005/70886; (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.143141-23-5,1-(Phenylsulfonyl)-7-azaindole,as a common compound, the synthetic route is as follows.

4.2.23 1-(Phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid (17) In a heat dried and nitrogen purged tricol round bottom flask, 5 (1.05 g, 4.07 mmol) was solubilized in dry THF (15 mL), cooled to -35 C then lithium diisopropylamide (5.1 mL, 10.16 mmol, 2 M) was added slowly. The mixture was then cooled to -55 C and dry ice was added slowly. The mixture was left to warm up to room temperature under stirring overnight. The reaction was quenched with water and extracted with EtOAC. The aqueous layer was acidified by the addition of a 6 N hydrochloric acid solution to pH = 1 and extracted with EtOAC. The latter organic layer was washed with a saturated sodium chloride solution, dried over magnesium sulfate, filtered and concentrated under reduced pressure to give 1.09 g of the expected product as a beige solid in 88% yield. 1H NMR (300 MHz, DMSO-d6) delta (ppm): 13.87 (br, 1H), 8.51 (dd, J = 1.6, 4.7 Hz, 1H), 8.26 (d, J = 7.0 Hz, 2H), 8.13 (dd, J = 1.6, 7.9 Hz, 1H), 7.77 (dd, J = 7.2 Hz, 1H), 7.72-7.65 (m, 2H), 7.39 (dd, J = 4.7, 7.9 Hz, 1H), 7.28 (s, 1H). 13C NMR (75 MHz, DMSO-d6) delta (ppm): 164.4, 149.5, 147.3, 138.5, 135.1, 133.3, 132.1, 129.8 (2C), 128.3 (2C), 121.1, 120.7, 112.5.

143141-23-5, As the paragraph descriping shows that 143141-23-5 is playing an increasingly important role.

Reference£º
Article; Baltus, Christine B.; Jorda, Radek; Marot, Christophe; Berka, Karel; Bazgier, Vaclav; Kry?tof, Vladimir; Prie, Gildas; Viaud-Massuard, Marie-Claude; European Journal of Medicinal Chemistry; vol. 108; (2016); p. 701 – 719;,
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

1211594-25-0, 4-Bromo-1H-indole-7-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 4-bromo-1H-indole-7-carboxylic acid (5.5 g, 22.91 mmol) EDC (6.59 g, 34.4 mmol) and HOBt (5.26 g, 34.4 mmol) in THF (150 mL) and DCM (180 mL) was stirred at rt for 1 h. The mixture was then bubbled with NH3 gas for about 15 mm and the resulting mixture was stirred at rt overnight. The mixture was diluted by addition of water and extracted with DCM. The organic phase was washed with brine, dried and concentrated to give a residue, which was suspended in ether and filtered to provide 4-bromo-]H-indole-7-carboxamide (5.3 g, 97%): ?H NMR (DMSO-d6) 3 11.40 (br, 1H), 8.08 (br, 1H), 7.29-7.57 (d, J = 7.6 Hz, 1H), 7.43-7.42 (m, 2H), 7.28-7.26 (d, J = 7.6 Hz, 1H), 6.43-6.42 (m, 1H).

1211594-25-0, 1211594-25-0 4-Bromo-1H-indole-7-carboxylic acid 59267539, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; ABBVIE INC.; BONAFOUX, Dominique; DAVIS, Heather, M.; FRANK, Kristine, E.; FRIEDMAN, Michael, M.; HEROLD, J., Martin; HOEMANN, Michael, Z.; HUNTLEY, Raymond; OSUMA, Augustine; SHEPPARD, George; SOMAL, Gagandeep, K.; VAN CAMP, Jennifer; VAN EPPS, Stacy, A.; VASUDEVAN, Anil; WALLACE, Grier, A.; WANG, Lu; WANG, Zhi; WILSON, Noel, S.; XU, Xiangdong; WO2014/210255; (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

15903-94-3, 6-(Benzyloxy)-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: General procedure for I catalyzed cascade Michael addition-hemiketalization reaction and the subsequent BF3¡¤Et2O promoted Friedel-Crafts alkylation reaction To a stirred solution of catalyst I (15 mol percent) and 2-((E)-2-nitrovinyl)phenols (8, 1 mmol) in toluene (2.5 mL), acetone (5 equiv, 5 mmol) was added. The resulting solution was stirred at 25 ¡ãC. After the reaction was complete (monitored by TLC), the reaction mixture was concentrated under reduced pressure and the crude product was purified by column chromatography on silica gel (200-300 mesh, PE/EtOAc=10/1) to afford the desired lactol intermediates 9 or open-chain compound 12. To a mixture of the obtained lactols 9 and indoles (10, 1.2 equiv) in acetonitrile (1 mL), BF3¡¤OEt2 (60 mol percent) was added portionwise at 25 ¡ãC. The resulting mixture was stirred at the same temperature for 10 h. The reaction mixture was concentrated in vacuo and the crude products were purified by column chromatography on silica gel (200-300 mesh, PE/EtOAc=10/1) to afford the desired 2-indolylchromanes 11. The title compounds were fully characterized by 1H NMR, 13C NMR, HRMS and specific rotation data. The enantiomeric excess of the pure products was determined by HPLC analysis using a chiral stationary phase.

15903-94-3, As the paragraph descriping shows that 15903-94-3 is playing an increasingly important role.

Reference£º
Article; Pan, Jianping; Wang, Yuehua; Chen, Shanren; Zhang, Xueqin; Wang, Youming; Zhou, Zhenghong; Tetrahedron; vol. 72; 1; (2016); p. 240 – 246;,
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.4792-67-0,Ethyl 5-chloro-1H-indole-2-carboxylate,as a common compound, the synthetic route is as follows.

[Referential Example 280] ethyl 3-bromo-5-chloroindole-2-carboxylate: N-Bromosuccinimide (440 mg) was added to a solution of ethyl 5-chloroindole-2-carboxylate (500 mg) in N,N-dimethylformamide (10 ml).. The reaction mixture was stirred at room temperature for 18 hours, and the solvent was distilled off under reduced pressure.. The residue was partitioned in ethyl acetate and water, and a water layer was extracted with ethyl acetate.. The resultant organic layers were combined, washed with saturated aqueous solution of sodium chloride and then dried over anhydrous sodium sulfate.. The solvent was distilled off, the residue was purified by column chromatagraphy on silica gel (ethyl acetate:hexane = 1:9), and white powder thus obtained was washed with hexane to obtain the title compound (680 mg).1H-NMR (CDCl3) delta: 1.42-1.48(3H,m), 4.43-4.49(2H,m), 7.30-7.32(2H,m), 7.65(1H,d,J=0.74Hz), 9.11(1H,s) MS (FAB) m/z: 303(M+H)+.

4792-67-0, The synthetic route of 4792-67-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1405852; (2004); 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

111258-23-2, Methyl 4-methoxy-1H-indole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,111258-23-2

(i) 3,7-Diiodo-4-methoxy-1H-indole-2-carboxylic acid methyl ester To a solution of 1 g 4-Methoxy-1H-indole-2-carboxylic acid methyl ester in 15 ml DCM, 5.4 g Bis(pyridine)iodonium(I) tetrafluoroborate were added at RT and the reaction was stirred over night. Then, the reaction mixture was diluted with 20 ml DCM and washed with sat. Na2S2O3 solution and water. The organic layer was separated and dried over Na2SO4 and the solvent removed under reduced pressure. The residue was used in the subsequent reaction without further purification. Yield: 1.6 g.

111258-23-2 Methyl 4-methoxy-1H-indole-2-carboxylate 688172, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Nazare, Marc; Essrich, Melanie; Will, David William; Matter, Hans; Ritter, Kurt; Wehner, Volkmar; US2003/199689; (2003); 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

610794-15-5, 4-Bromo-5-methyl-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

610794-15-5, 4-Bromo-5-methylindole (0.7 g, 3.35 mmol), bis(pinacolato)diboron (1.7 g, 6.7 mmol), KOAc (1 g, 10 mmol) and Pd(dppf)Cl2 (73 mg, 3 mol %) were suspended in dry DMSO (20 mL) in two 40 mL glass tubes which were tightly sealed with an aluminium/Teflon crimp. The samples were irradiated at 250 W, 180 C. for 40 min in a CEM-Discover mono-mode microwave reactor. After completion of the reactions, the vessels were cooled down to 60 C., combined and the crude mixture was filtered through a thin plug of celite. The celite plug was washed with EtOAc (50 mL), the organic fractions were combined and the solvent was removed under reduced pressure. The crude product was purified by silica gel column chromatography and then prep-HPLC to give 5 (280 mg, 33%). 1H NMR CDCl3400 MHz delta 1.41 (s, 12H), 2.63 (s, 3H), 6.96-6.97 (m, 1H), 7.01-7.03 (m, 1H), 7.18-7.20 (m, 1H), 7.32-7.34 (m, 1H), 8.13 (s, 1H)

As the paragraph descriping shows that 610794-15-5 is playing an increasingly important role.

Reference£º
Patent; SAREUM LIMITED; Reader, John Charles; US2015/18367; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.90271-86-6,5-Bromo-3-cyanoindole,as a common compound, the synthetic route is as follows.

General procedure: To a cold solution of the appropriate indoles 4a-d (4.2 mmol) in anhydrous DMF (7.8 mL) NaH(60% suspension in mineral oil, 6.3 mmol, 0.25 g) was added. After 30 min stirring at room temperature,tert-butyl (2-bromoethyl)carbamate [42] (6.3 mmol, 1.4 g) was added. The reaction mixture was heatedat 60 C for 24 h. After cooling, the mixture was poured into ice-water and extracted with ethyl acetate(3 20 mL). The organic phases were dried (anhydrous Na2SO4) and evaporated under reducedpressure. The residue was purified by column chromatography using petroleum ether/ethyl acetate(70/30) (for 5b-d) or petroleum ether/ethyl acetate (50/50) (for 5a) as eluent., 90271-86-6

As the paragraph descriping shows that 90271-86-6 is playing an increasingly important role.

Reference£º
Article; Carbone, Anna; Parrino, Barbara; Cusimano, Maria Grazia; Spano, Virginia; Montalbano, Alessandra; Barraja, Paola; Schillaci, Domenico; Cirrincione, Girolamo; Diana, Patrizia; Cascioferro, Stella; Marine Drugs; vol. 16; 8; (2018);,
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

143612-79-7, 3-(4-Chlorobutyl)-1H-indole-5-carbonitrile is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

under nitrogen protection,A commercially available 6.8 g of 3- (4-chlorobutyl) -5-cyanoindole was dissolved in 70 mL of ether with 8.9 g of cuprous iodide to form a reaction solution,Heated to reflux for 3.5 hours.Then the commercially available 5.9g5-piperazine-benzofuran 2-carboxylate and60 g of sodium methoxide was added to the stirred reaction solution,The reaction solution was reacted at 90 C for 5.5 hours until TLC was complete.The reaction solution was cooled to room temperature and poured slowlyStirring in 100 mL of aqueous potassium hydroxide solution, a large amount of yellow solid precipitated and precipitatedThe solid reaction solution was stirred for 1 hour and then filtered to obtain a filter cake which was washed with 50 mL of waterAfter three runs, 8.9 g of 5- (4- [4- (5-cyano-3-indolyl) -butyl] -1-piperazinyl)Benzofuran-2-carboxylate., 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; Suzhou Uugene Biopharma Co., Ltd.; Hu, Fan; Wang, Shenyong; Shao, Changkun; Li, Sheng; Wang, Xiaojun; Hu, Junkai; (12 pag.)CN103360373; (2016); B;,
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.1015460-59-9,7-Bromo-5H-pyrido[4,3-b]indole,as a common compound, the synthetic route is as follows.

Step 3: 7-(6-Fluoropyridin-3-yl)-5H-pyrido[4,3-b]indole A mixture of 7-bromo-5H-pyrido[4,3-b]indole (400 mg, 1.63 mmol), (6-fluoropyridin-3-yl)boronic acid (344 mg, 2.44 mmol), PdCl2(dppf) (120 mg, 0.163 mmol), tBu3PHBF4 (95 mg, 0.326 mmol) and Cs2CO3 (1.1 g, 3.26 mmol) in dioxane/water (20 mL, 20:1) was heated to 90 C. for 4 hours under N2. The solid was filtered and the filtrate was evaporated. The residue was purified by chromatography (silica gel, 200-300 mesh, CH2Cl2: MeOH=30:1) to afford 7-(6-Fluoropyridin-3-yl)-5H-pyrido[4,3-b]indole (250 mg, 59% yield).

1015460-59-9, 1015460-59-9 7-Bromo-5H-pyrido[4,3-b]indole 71079324, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Arvinas, Inc.; Crew, Andrew P.; Berlin, Michael; Flanagan, John J.; Dong, Hanqing; Ishchenko, Alexey; (559 pag.)US2018/125821; (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