Month: September 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.105191-12-6,6-Bromo-1H-indole-2-carbaldehyde,as a common compound, the synthetic route is as follows.

General procedure: To a mixture of 1H-indole-2-carbaldehyde (290 mg, 2.0 mmol, 1.0 eq.) and 1-(5-bromo-2-hydroxyphenyl)ethanone (430 mg, 2.0 mmol, 1.0 eq.) in ethanol (10 mL) was added piperidine (1 mL). The mixture was refluxed during 16 hours and then diluted with ethyl acetate after cooling to room temperature. The organic layer was washed with a 1M aqueous hydrochloric acid solution and water, dried over Na2SO4and then evaporated under reduced pressure. The residue was purified by silica gel flash-column chromatography (eluent: heptane/EtOAc, 90/10 to 80/20) to afford, after trituration with diethyl ether,7aas a red solid (160 mg, 23 %).

105191-12-6, The synthetic route of 105191-12-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Labriere, Christophe; Gong, Huansheng; Finlay, B. Brett; Reiner, Neil E.; Young, Robert N.; European Journal of Medicinal Chemistry; vol. 125; (2017); p. 1 – 13;,
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

272-49-1, 4-Azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

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

The synthetic route of 272-49-1 has been constantly updated, and we look forward to future research findings.

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

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

6-Hydroxy-2,3-dihydro-isoindol-1-one6-Methoxy-2,3-dihydro-isoindol-1-one (90 g, 0.55 moles, 1 equiv) was suspended in 2.52 L of DCM and 661 mL of BBr3 ( 0.66 moles, 1.2 equiv, 1.0 M solution in DCM) was added over 2 h at 0 0C. After the addition was complete, the reaction mixture was allowed to warm to room temperature over 3 h then stirred overnight. The reaction mixture was quenched by the addition of 1 L of MeOH at 0 0C and then stirred at room temperature for 3 h.Solvent was evaporated under vacuum, and the crude material was triturated with minimum amount of MeOH (-400 mL). The solid was filtered and dried under vacuum at 50 0C for 24 h to give 46.3 g of 6-Hydroxy-2,3-dihydro-isoindol-1-one with >98 % purity (56%). The mother liquor was concentrated and triturated with minimum amount of MeOH to afford 32 g of additional 6-Hydroxy-2,3-dihydro-isoindol-1-one with >90 % purity (39%).

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

Reference£º
Patent; PFIZER PRODUCTS INC.; WO2008/20306; (2008); A2;,
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.107516-75-6,Diethyl 1H-indole-2,6-dicarboxylate,as a common compound, the synthetic route is as follows.

Example 5 Synthesis of (R)-3-aminomethyl-1-oxo-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole-7-carboxylic acid pyridin-3-ylamide A mixture of K2CO3 (1.06 g, 7.65 mmol) and 1H-indole-2,6-dicarboxylic acid diethyl ester (1.0 g, 3.8 mmol) in DMF (15 mL) was stirred at room temperature for 0.5 h. Then toluene-4-sulfonic acid (S)-2,2-dimethyl-[1,3]dioxolan-4-yl methyl ester (1.20 g, 4.2 mmol) in DMF (5 mL) was added. The reaction mixture was warmed to 100 C. and kept at this temperature overnight. The reaction was concentrated and the residues were extracted with EtOAc several times. The combined organic extracts were washed with brine, dried over MgSO4 and concentrated. Purification by silica gel chromatography gave 1.34 g of 1-((R)-2,2-dimethyl-[1,3]dioxolan-4-ylmethyl)-1H-indole-2,6-dicarboxylic acid diethyl ester as white solid, yield 93%. ESI-MS m/z 376.42 [M+H]+.

107516-75-6, The synthetic route of 107516-75-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Boehringer Ingelheim Pharmaceuticals, Inc.; US2006/276453; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.399-52-0,5-Fluoro-1H-indole,as a common compound, the synthetic route is as follows.,399-52-0

General procedure: A method for synthesizing compound III-1 wherein R1, R2 and R3 are simultaneously hydrogen in the formula III, the method comprising the steps of:(1) Add to a 50 mL round bottom flask1.0mmol indole(In the formula I, R1, R2, and R3 are both hydrogen) and1.0 mmol (0.140 g) of hexamethylenetetramine, then 2 mL of N,N-dimethylformamide (DMF), stirred in a magnetic stirrer to dissolve the solid, followed by the addition of 0.05 mmol (0.012 g) of crystalline trichloride Aluminum, connected to a reflux condenser, heated at 120 C, the reaction progress was monitored by TLC, and the reaction was cooled to room temperature after 1 h to prepare a suspension;(2) The suspension prepared in the step (1) is suction filtered with a funnel padded with diatomaceous earth.The filter cake was washed well with ethyl acetate, suction filtered, and the above operation was repeated until the filtrate had no product, and all the filtrates were combined.Dilute with 15 mL of saturated saline solution, disperse and separate the layers, and the aqueous layer was further extracted with ethyl acetate three times.Each time 10 mL, the ethyl acetate layer was combined and washed with 10 mL of 2 mol/L diluted hydrochloric acid.Wash with 10 mL of saturated sodium bicarbonate solution, and finally wash with 10 mL of saturated brine.The washed ethyl acetate layer was dried over anhydrous sodium sulfate, and after drying, the desiccant was filtered off.Then use a rotary evaporator to recover the solvent to concentrate the product, and finally,The residue is subjected to silica gel column chromatography using a mixture of n-hexane-ethyl acetate (V/V = 2:1) as an eluent to obtain a purified product.The mass of the compound III-indole-3-carbaldehyde is 0.137g,The product yield was 94%.

The synthetic route of 399-52-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Yancheng Jin Ming Pharmaceutical Co., Ltd.; Yancheng Normal College; Wang Qingdong; Yang Zijian; Fang Yue; Wu Zhen; Zeng Bubing; Yang Jinming; Hu Chaojun; Zhao Yujun; (19 pag.)CN108329249; (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

1224724-39-3, Methyl 4-bromo-1H-indole-7-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a mixed solution of compound 267c (800 mg, 3.149 mmol) in methanol (6 mL) and tetrahydrofuran (6 mL) was added a solution of lithium hydroxide in water (12 mL) at room temperature. The mixture was stirred at room temperature for 2.5 hours. The reaction solution was concentrated under reduced pressure, water was added to the residue and neutralized with dilute hydrochloric acid, and then extracted with ethyl acetate (80 mL ¡Á 3).The organic phases were combined, washed with saturated brine, and dried over anhydrous sodium sulfate. The filtrate was concentrated under reduced pressure, ethyl acetate and petroleum ether were added to the residue, and the white solid compound 267d, 4-bromo-1H-indole-7-carboxylic acid (360 mg, 44.8% yield) was collected by filtration.

1224724-39-3, As the paragraph descriping shows that 1224724-39-3 is playing an increasingly important role.

Reference£º
Patent; Jiaxing Tekeluo Biological Technology Co., Ltd.; Xing Li; Li Guanqun; Wang Xiaolei; Cai Yuting; Jiang Xiang; Pan Xiang; Zhu Wenhao; Wang Yang; Wang Zengquan; (83 pag.)CN110627775; (2019); 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.883535-89-5,2-(2-Methyl-1H-indol-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

883535-89-5, A solution of 2-(2-methyl-1H-indol-1-yl)ethanamine (4a) (65 mg, 0.373 mmol) and 4-(piperidin-1-yl)benzoic acid (5) (76 mg, 1 eq.), and dimethylaminopyridine (catalytic, ?5 mg) in dichloromethane (6 mL) was added 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide.hydrochloride (EDCI) (92 mg, 1.3 eq.) at room temperature. The resulting reaction mixture was stirred for 6h. At the conclusion of the reaction (TLC), water (15 mL) was added to quench the reaction. The product was extracted with ethyl acetate (20mL¡Á3). Organics were washed with dilute HCl (10 mL), saturated NaHCO3 solution (10 mL), water (10 mL) and brine solution (10 mL) and dried over Na2SO4 and concentrated. The resulting crude product was subjected to silica gel chromatography eluting with 0-40% ethyl acetate in hexane to furnish 7k (TG7-152) (100mg, 74% yield). 1H NMR (CDCl3): delta 7.52 (d, J=5.6Hz, 1H), 7.49 (d, J=8.8Hz, 2H), 7.30 (d, J=8Hz, 1H), 7.07 (m, 2H), 6.80 (d, J=8.2Hz, 2H), 6.23 (s, 1H), 5.98 (t, J=5.4Hz, 1H), 4.33 (t, J=6Hz, 2H), 3.76 (q, J=6Hz, 2H), 3.25 (t, J=4.8Hz, 4H), 2.37 (s, 3H), 1.6 (m, 6H). LCMS (ESI): >97% purity at lambda 254, MS; m/z, 362 [M+H]+. Anal. Calcd. for C23H27N3O: C, 76.42; H, 7.53; N, 11.62; found; C, 76.48; H, 7.55; N, 11.59.

As the paragraph descriping shows that 883535-89-5 is playing an increasingly important role.

Reference£º
Article; Ganesh, Thota; Jiang, Jianxiong; Dingledine, Ray; European Journal of Medicinal Chemistry; vol. 82; (2014); p. 521 – 535;,
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

408355-23-7, 7-Bromo-5-fluoro-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,408355-23-7

Combine N-(2-(lH-l,2,3-triazol-l-yl)ethyl)-5-fluoro-4-(7-(4,4,5,5- tetramethyl-l,3,2-dioxaborolan-2-yl)benzo[b]thiophen-2-yl)pyrimidin-2-amine (0.12 g, 0.26 mmol), 7-bromo-5-fluoro-lH-indole (64 mg, 0.28 mmol, synthesized based on reference: Manfred S.; Assunta G.; Frederic L., Eur. J. Org. Chan. 2006, 2956- 2969), barium hydroxide octahydrate (0.24 g, 0.77 mmol, alternatively sodium carbonate, potassium carbonate, cesium fluoride), Pd(dppf)Ci2 (20 mg, 0.03 mmol) in 2 mL of mixed solvent of DMF (alternatively dioxane, DMSO) and water (4/1, v/v). Purge the mixture with nu2 three times. Heat the reaction mixture to 80 0C for 4 h (HPLC monitor) (or microwave reactor). Cool to RT. Dilute with chloroform/IPA (3: 1, v/v) 50 mL. Wash with water, aqueous saturated sodium chloride and dry over magnesium sulfate. Remove the organic solvent to give the crude product. Purify the residue by column chromatography (hexane to ethyl acetate, or methylene chloride and methanol) to give the title compound (0.053 g, 43 %). MS (ES) m/z 474 [M+ 1]+.

408355-23-7 7-Bromo-5-fluoro-1H-indole 3852879, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; ELI LILLY AND COMPANY; WO2008/144223; (2008); A2;,
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

23077-44-3, 6-Fluoro-1H-indole-3-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

DMF (0.1 mL) was added to a stirring mixture of 6-fluoroiindole-3- carboxylic acid (3.500 g, 19.5 mmol, l .Oequiv.) and oxalyl chloride (3.306 ml, 39.1 mmol, 2.0 equiv.) in dichloromethane (40 mL) under nitrogen at 0oC(ice bath tmeperature). After 2 hours the reaction was concentrated to dryness. The residue was taken up in DCM (20 mL) and cooled to 0C and tropine (8.276 g, 58.6 mmol, 3.0 equiv.) was added as a solution in DCM (25mL) with stirring. The reaction mixture was allowed to come to room temperature and stirred overnight. The reaction mixture was washed with saturated sodium bicarbonate and the solvents removed under reduced pressure. The residue was titurated with ethyl acetate and hexanes to get the product as a tan colored solid (2.34g, 39.6%). 1H MR (DMSO-d6, 300 MHz): 11.94 (s, 1H), 8.01-7.96 (m, 2H), 7.27 (dd,J=9.9 & 2.4 Hz, 1H), 7.08-7.01 (m, 1H),5.06 (t, J=5.4 Hz, 1H), 3.09 (s, 2H), 2.21 -1.99 (m, 9H), 1.75-1.70 (m, 2H). LC/MS: 303.6 (M+l).

23077-44-3, 23077-44-3 6-Fluoro-1H-indole-3-carboxylic acid 28806318, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; BUCK INSTITUTE FOR RESEARCH ON AGING; JOHN, Varghese; BREDESEN, Dale, E.; SPILMAN, Patricia, R.; JAGODZINSKA, Barbara; (85 pag.)WO2017/197177; (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.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

As the paragraph descriping shows that 272-49-1 is playing an increasingly important role.

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