Day: November 5, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1912-33-0,Methyl 2-(1H-indol-3-yl)acetate,as a common compound, the synthetic route is as follows.

(2) in a 500 ml round bottom flask methyl indole acetic acid is added in 9.46g (48mmol), ethylene glycol monomethyl ether (40 ml), 5 ml of hydrazine hydrate, 115 ¡ãC heating reflux reaction about 20 hours, thin layer chromatography (TLC) detecting raw material point dematerialised, stop the reaction, cooling to room temperature, adding water (50 ml), static separating white solid, filtering to get the crude product, using ethanol is recrystallized to get indole acetic acid hydrazide white solid 9.2 g.

1912-33-0, As the paragraph descriping shows that 1912-33-0 is playing an increasingly important role.

Reference£º
Patent; Kunming University of Science and Technology; Yunnan University; Xia, Xueshan; He, Yanping; Feng, Yue; Fan, Mengran; Gao, Fengpin; Zhang, Yufang; Li, Cong; (21 pag.)CN105732468; (2016); 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

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

Compound 3 (233 g, 1.0mol) and 6 (245 g, 1.0 mol) were dissolved in acetonitrile (3 L), and then, triethylamine (101 g, 1.0mol) and K2CO3 (138g,1.0mol) were added to the solution. The mixture was heated at reflux for 12 h. Subsequently, the reaction mixture was poured into cold water (3L). After filtration, the solid was dissolved in EtOAc, and then, HCl-EtOAc saturated solution was added to enable crystallization. Product 7 was obtained as a white solid. Yield 287 g (65%) with 99% HPLC purity after the mixture was filtered. m.p. 276.5-279.2C (Lit1 277-279C). 1H NMR (400MHz, DMSO-d6): delta 11.35 (s, 1H), 8.04 (d, J=18.3Hz, 2H), 7.74-6.88 (m, 8H), 3.69-3.15 (m, 8H), 2.74 (t, J= 7.2Hz, 2H), 2.37 (t, J =7.2Hz, 2H), 1.80-1.61 (m, 2H), 1.54 (d, J=6.8Hz, 2H). 13C NMR (100 MHz, DMSO-d6): delta 159.9, 148.8, 147.9, 138.6, 137.7, 127.8, 126.9, 124.7, 124.0, 123.3, 120.9, 117.8, 115.7, 112.4, 111.6, 109.5, 107.3, 100.0, 57.5, 52.8(2), 49.8(2), 27.7, 26.1, 24.1. HRMS (ESI): m/z [M+H]+ calculated for C26H27N5O2: 442.2238, found: 442.2240.

143612-79-7, As the paragraph descriping shows that 143612-79-7 is playing an increasingly important role.

Reference£º
Article; Hu, Fan; Su, Weike; Journal of Chemical Research; vol. 44; 3-4; (2020); p. 243 – 247;,
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.

Intermediate 48: Synthesis of 3-(4-azetidin-l-ylcyclohex-l-en-l-yl)-li/-pyrrolo[3,2- b] pyridine1. Synthesis of 3-(l,4-dioxaspiro[4.51dec-7-en-8-yl)-lH-pyrrolo[3,2-blpyridine.Potassium hydroxide (41.0 mmol) was added to a mixture of 4-azaindole (13.5 mmol) and 1 ,4-cyclohexanedione monoethylene acetal (13.5 mmol) in methanol (30 mL) and the reaction mixture was heated at reflux for 4h. The reaction mixture was diluted with ice water(200 mL) and the precipitated solids were collected by filtration, washed with water, and air dried. The residue was purified by Flash chromatography (70/30 to 50/50 hexane/ethyl acetate) to provide 3-(l,4-dioxaspiro[4.5]dec-7-en-8-yl)-lH-pyrrolo[3,2-b]pyridine. Data: 1H NMR (CDCl3) 6 8.51 (dd, J= 4.7, 1.4, IH), 8.15 (br, IH), 7.63 (dd, J= 8.2, 1.4, IH), 7.36 (s, IH), 7.15(m, IH), 7.11 (dd, J = 8.2, 4.7, IH), 4.03 (s, 4H), 2.8-2.6 (m, 2H), 2.6-2.4 (m, 2H), 1.8-2.2 (m,2H).

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

Reference£º
Patent; MEMORY PHARMACEUTICALS CORPORATION; SCHUMACHER, Richard, A.; TEHIM, Ashok; XIE, Wenge; WO2010/24980; (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.35320-67-3,2-Methyl-1H-indol-4-ol,as a common compound, the synthetic route is as follows.

Reference example19 2-methyl-1H-indol-4-yloxyphenylmethyl acetic acid benzyl ester Under argon gas, potassium carbonate (2.14g) and bromoacetic acid benzyl (1.08ml) were added to N, N-dimethyl formamide (10ml) solution containing 4-hydroxy-2-methyl-1H-indole (612mg), which was stirred at 60C for 1hour.. water was added to the reactive mixture, which was extracted by ethyl acetate.. The organic layer was sequentially washed with water and saturated brine, and then dried by anhydrous sodium sulfate.. The residue obtained by removal of the solvent was recrystallized by ethylacetate-hexane to give a title compound (1.3g) having the following physical properties. TLC:Rf 0.45 (hexane: ethyl acetate=7:3); NMR(CDCl3):delta 7.87 (brs, 1H), 7.40-7.30 (m, 5H), 7.01-6.94 (m, 2H), 6.44-6.36 (m, 2H), 5.25 (s, 2H), 4.80 (s, 2H), 2.43 (s, 3H)., 35320-67-3

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; ONO PHARMACEUTICAL CO., LTD.; EP1424325; (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

1953-54-4, 5-Hydroxyindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: N-phenyl glyoxylamide 1a (1.0 mmol), indole 2a (1.1 mmol), and 20 mmol% FeSO4 were added to 6 mL of C2H5OH and then the mixture was stirred at room temperature for 0.5 h. After the completion of the reaction (monitored by TLC analysis), the mixture was diluted with water and extracted with ethyl acetate (20 mL ¡Á 4). The organic layer was washed with saturated brine, dried over anhydrous sodium sulfate and the solvent was evaporated to dryness. The crude residue was purified by flash chromatography on silica (dichloromethane/methanol=80/1) to afford pure 2-hydroxy-2-(1H-indol-3-yl)-N-phenylacetamide 3a as a yellow solid (247.6 mg, 93% yield)., 1953-54-4

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

Reference£º
Article; Zheng, Yang; Li, Ren-Jun; Zhan, Zhen; Zhou, Yan; Hai, Li; Wu, Yong; Chinese Chemical Letters; vol. 27; 1; (2016); p. 41 – 46;,
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.

To a mixture of 1H-pyrrolo[3,2-b]pyridine (Purchased from Combi Blocks Inc.), (5 g) and DMF (100 mL) stirred under nitrogen at room temperature was added potassium hydroxide (9.02 g) followed by iodine (12.89 g) and the resulting mixture was stirred at room temperature for 1 h 5 min., then poured onto a mixture of Na2S2O5.5H2O (4.25 g), water (635 mL), and 28-30percent ammonium hydroxide (43 mL). The resultant mixture was cooled in an ice bath for 20 min, and the precipitate thus produced was filtered and washed with ice water then dried under vacuum to give the title compound (9.18 g). LCMS: m/z 245.39 [M+H]+. 1H NMR (400 MHz, DMSO-d6) ppm 7.17 (dd, J=8.1, 4.5 Hz, 1H) 7.72-7.87 (m, 2H) 8.38 (d, J=4.4 Hz, 1H) 11.74 (br. s., 1H)

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

Reference£º
Patent; EISAI R&D MANAGEMENT CO., LTD.; PAYNE, Andrew; CASTRO PINEIRO, Jose Luis; BIRCH, Louise Michelle; KHAN, Afzal; BRAUNTON, Alan James; KITULAGODA, James Edward; SOEJIMA, Motohiro; WO2015/49574; (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

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

Ethyl 5-fluoro-1H-indole-2-carboxylate (2 g, 9.7 mmol) and 1H-pyrrole-2,5-dione (1.40 g, 14.4 mmol)were added to dry 1,2-dichloroethane (50 mL), and 46.5% BF3-Et2O (3.54 g, 11.6 mmol) was added toreaction mixture at 20 C. After the reaction mixture was stirred at 90 C, until the starting materialdisappeared in thin layer chromatography (TLC), the reaction mixture was distilled in vacuo, anddichloromethane (50 mL) was added to the mixture. The organic extract was washed twice withsaturated aqueous NaHCO3 and NaCl (20 mL) respectively, and the organic extract was dried overNa2SO4. After solvent was removed under vacuum, the product was purified as a white solid bysilica gel column chromatography, 1.62 g, yield 55%. 1H-NMR (400 MHz, DMSO-d6): = 12.00 (s, 1H,NH-indolyl), 11.31 (s, 1H, NH), 7.49-7.45 (m, 2H, H-indolyl), 7.18 (td, J = 9.2, 2.6 Hz, 1H, H-indolyl),4.82 (dd, J = 9.6, 6.6 Hz, 1H, CH), 4.33-4.27 (m, 2H, CH2), 3.08 (dd, J = 17.7, 9.6 Hz, 1H, CH?H?), 2.70(dd, J = 17.7, 6.6 Hz, 1H, CH?H?), 1.30 (t, J = 7.1 Hz, 3H, CH3). 13C-NMR (101 MHz, CD3OD): =182.17,180.15, 162.66, 160.66, 134.24, 129.01, 126.54, 119.11, 115.66, 114.82, 104.78, 62.19, 39.68, 39.37, 14.63.HRMS (ESI): m/z [M + H]+ calculated for C15H14O4N2F: 305.09321; found: 305.09290.

348-36-7, The synthetic route of 348-36-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Wen, Hui; Liu, Yuke; Wang, Shufang; Wang, Ting; Zhang, Gang; Chen, Xiaoguang; Li, Yan; Cui, Huaqing; Lai, Fangfang; Sheng, Li; Molecules; vol. 24; 11; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.16732-70-0,Ethyl 5-bromo-1H-indole-2-carboxylate,as a common compound, the synthetic route is as follows.

A solution of the 3a (0.204 g, 0.5 mmol), ethyl 5-bromo-1Hindole-2-carboxylate (0.134 g, 0.5 mmol), Pd(dppf)2Cl2 (0.018 g,0.025 mmol) and Cs2CO3 (0.33 g, 0.56 mmol) in DMF (10 ml) underan atmosphere of N2 was stirred at 90 C for 4 h. DMF was removedunder reduced pressure and the residue was purified through acolumn chromatography on silica with chloroform/methanol (V:V20:1) as a white solid (0.12 g, 51.2% yield). mp 108-110 C. 1H NMR(400 MHz, DMSO) delta 12.00 (s, 1H, NH), 10.02 (s, 1H, NH), 8.27 (d,J 2.2 Hz, 1H, Ar-H), 7.87-7.80 (m, 4H, Ar-H), 7.55 (d, J 8.6 Hz, 1H,Ar-H), 7.49 (dd, J 8.6, 1.4 Hz, 1H, Ar-H), 7.43 (t, J 8.8 Hz, 2H, Ar-H), 7.22 (d, J 1.5 Hz, 1H, Ar-H), 4.36 (q, J 7.1 Hz, 2H, CH2), 3.66 (s,3H, CH3), 1.36 (t, J 7.1 Hz, 3H, CH3).13C NMR (100 MHz, DMSO)delta 164.8 (J 249.7 Hz), 161.7, 156.4, 141.6, 137.4, 137.1, 137.0, 132.3,131.1, 130.3 (d, J 9.6 Hz), 129.2, 128.7, 127.8, 124.2, 120.6, 120.2,116.7 (d, J 22.8 Hz), 113.8, 108.5, 61.0, 53.8, 14.8. HRMS: m/z470.1181 [MH]., 16732-70-0

As the paragraph descriping shows that 16732-70-0 is playing an increasingly important role.

Reference£º
Article; Fan, Yan-Hua; Li, Wei; Liu, Dan-Dan; Bai, Meng-Xuan; Song, Hong-Rui; Xu, Yong-Nan; Lee, SangKook; Zhou, Zhi-Peng; Wang, Jian; Ding, Huai-Wei; European Journal of Medicinal Chemistry; vol. 139; (2017); p. 95 – 106;,
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

875-30-9, 1,3-Dimethyl-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Under argon atmosphere,To a dry Schlenk tube were added sequentially tetrabutylammonium borofluoride copper (0.0025 mmol)(R) -XylBINAP (0.0015 mmol)And dry m-xylene (0.25 mL),After stirring at room temperature for 20 minutes, 1,3-dimethylindole (0.05 mmol dissolved in 0.25 mL of dry m-xylene)And 2- (4-tert-butylphenyl) -N-p-toluenesulfonylimidazine (0.11 mmol),After completion of the reaction was stirred at 15 C for 12 hours (TLC monitoring).The reaction was quenched by the addition of saturated aqueous sodium bicarbonate (5 mL), extracted with ethyl acetate (5 mL x 3), dried over anhydrous magnesium sulfate and the solvent removed under reduced pressure to give the crude product which was analyzed by 1H NMR for its diastereomer The proportion of dr> 20: 1, a mixed solvent of petroleum ether: ethyl acetate = 20: 1 (containing 0.5v% triethylamine) as developing solvent,The product was isolated by column chromatography (23.3 mg, yield: 98%, e.r. = 98.5: 1.5).

875-30-9, The synthetic route of 875-30-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Anhui Normal University; Chai Zhuo; Zhu Youmin; Wang Shaowu; Yang Peijun; Yang Gaosheng; (18 pag.)CN104804004; (2017); 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.32387-18-1,1-(5-Bromo-1H-indol-3-yl)-2,2,2-trifluoroethanone,as a common compound, the synthetic route is as follows.

General procedure: One of compounds 3a-3f (20 mmol) was dissolved in DMF (10 mL). Trifluoroacetic anhydride (4.2 mL, 30 mmol) was added dropwise at 0C. After stirring for 3.5 h, water was added, the solid filtered off and treated with 20% NaOH (40 mL, 0.2 mol) at 55C overnight. Upon cooling down, the solution was extracted with Et2O. The aqueous phase was acidified with concentrated HCl and the residue was filtered off to give one of compounds 4a-4f., 32387-18-1

As the paragraph descriping shows that 32387-18-1 is playing an increasingly important role.

Reference£º
Letter; Zhang; Xu; Wang; Kang; Russian Journal of General Chemistry; vol. 87; 12; (2017); p. 3006 – 3016;,
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