Day: November 17, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.6245-89-2,(1H-Indol-3-yl)-1-propanamine,as a common compound, the synthetic route is as follows.

6245-89-2, Proceeding as in Example 3, but replacing 2-[2-(cyclopropylmethyloxy)phenoxy]ethyl methanesulfonate with 2-(2-ethyloxyphenoxy)ethyl methanesulfonate and [2-(5-chloro-1H-indol-3-yl)-1,1-dimethylethyl]amine with [3-(1H-indol-3-yl)-prop-1-yl]amine, gave [3-(1H-indol-3-yl)prop-1-yl][2-(2-ethyloxyphenoxy)ethyl]amine hydrochloride, m.p. 147¡ã-148¡ã C.

As the paragraph descriping shows that 6245-89-2 is playing an increasingly important role.

Reference£º
Patent; Syntex (U.S.A.) Inc.; US5436264; (1995); 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

198479-63-9, 5-(Benzyloxy)-2-(4-(benzyloxy)phenyl)-3-methyl-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The indole (5) dissolved in THF (10 mL) was added dropwise toa stirring mixture of NaH in THF (10 mL) at 0 C under N2 atmosphere.The mixture was stirred for 10 min, at which point theappropriate dibromoalkane (6)-(10) was added and the mixturewas stirred for 30 min at 0 C. The reaction was refluxed for a further30 min under N2 atmosphere, the mixture was allowed to coolat which point water was added dropwise until the solutionbecame clear. The solvent was then evaporated under reducedpressure to obtain a brown oil. The resin was dissolved in DCM(50 mL) and washed with water (3 50 mL), brine (50 mL) anddried over Na2SO4. The solvent was evaporated under reducedpressure to obtain a brown oil. The material was purified via flashchromatography over silica gel to afford the desired product., 198479-63-9

As the paragraph descriping shows that 198479-63-9 is playing an increasingly important role.

Reference£º
Article; Kelly, Patrick M.; Bright, Sandra A.; Fayne, Darren; Pollock, Jade K.; Zisterer, Daniela M.; Williams, D. Clive; Meegan, Mary J.; Bioorganic and Medicinal Chemistry; vol. 24; 18; (2016); p. 4075 – 4099;,
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

344790-96-1, 5-Bromo-4-fluoro-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5-Bromo-4-fluoro-1H-indole obtained by the method described in Eur. J. Org. Chem. 2956-2969, 2006 (793 mg) was dissolved in N,N-dimethylformamide (30 ml), and bis(pinacolato)diboron (1.88 g), potassium acetate (1.82 g) and a [1,1′-bis(diphenylphosphino)ferrocene]palladium(II) chloride-dichloromethane complex (151 mg) were added. The mixture was stirred with heating under nitrogen atmosphere at 100 C. overnight. The reaction solution was cooled to room temperature and then concentrated under reduced pressure. The residue was purified by silica gel column chromatography (developed with ethyl acetate-hexane). The resulting colorless oil was slurry washed with hexane to give the title compound (481 mg) as a colorless solid.MS (EI) m/z: 261M+.1H-NMR (CDCl3) delta: 1.38 (12H, s), 6.65-6.68 (1H, m), 7.14-7.17 (1H, m), 7.18 (1H, s), 7.51 (1H, dd, J=8.3, 5.5 Hz), 8.27 (1H, brs).

344790-96-1, The synthetic route of 344790-96-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Daiichi Sankyo Company, Limited; US2011/82138; (2011); 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.6146-52-7,5-Nitroindole,as a common compound, the synthetic route is as follows.

6146-52-7, General procedure: A 50 mL round-bottomed flask equipped with a magnetic stirringbar was charged with the appropriate indole 1 (0.5 mmol,1.0 equiv), 37% aq HCHO (0.5 mmol, 0.0406 g, 1.0 equiv), 25% aqNH3 (1.0 mmol, 0.0681 g, 2.0 equiv), FeCl3 (0.01 mmol, 0.0016 g,2 mol%), and DMF (2 mL). The flask was fitted with a reflux condenser,and the mixture was stirred at 130 C under open air.When the reaction was complete (TLC), the mixture was cooledto r.t., diluted with sat. aq NaCl (10 mL) and 0.5 M aq HCl (2 mL),and extracted with EtOAc (3 x 7 mL). The organic layers werecombined, washed with sat. aq NaHCO3 (10 mL) and sat. aq NaCl(10 mL), dried (Na2SO4), and concentrated under reduced pressure.The residue was purified by flash column chromatography(silica gel, hexane-EtOAc).

6146-52-7 5-Nitroindole 22523, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Wang, Qing-Dong; Zhou, Bin; Yang, Jin-Ming; Fang, Dong; Ren, Jiangmeng; Zeng, Bu-Bing; Synlett; vol. 28; 19; (2017); p. 2670 – 2674;,
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.

Description for D11; 1H-indole-6-carbaldehyde oxime (D1); Hydroxylamine hydrochloride (0.574 g) was added portionwise to a solution of 1H-indole-6-carbaldehyde (1 g) in pyridine (5 ml) are RT. The resulting solution was heated to reflux and stirred at that temperature for 1 hour. The solvent was evaporated. The residue was diluted with ethyl acetate (50 mL) and the resulting solution was washed with aqueous hydrochloric acid (0.5 M, 40 mL). The organic fraction was separated and dried over anhydrous magnesium sulfate. The dried solution was concentrated to afford a brown oily solid. The residue was triturated with ether/hexane to afford 1H-indole-6-carbaldehyde oxime (D11) as a pink solid (128 mg). Solid was precipitated out from the filtrate. The solid was collected to give another batch of 1H-indole-6-carbaldehyde oxime (D11) (818 mg). deltaH (DMSO-d6, 400 MHz): 6.44 (1H, m), 7.24 (1H, dd), 7.32 (1H, m), 7.55 (1H, dd), 7.57 (1H, s), 8.19 (1H, s), 10.88 (1H, s), 11.25 (1H, brs)., 1196-70-9

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

Reference£º
Patent; Castro Pineiro, Jose Luis; Lin, Xichen; Liu, Qian; Meng, Kevin; Ren, Feng; Vesey, David R.; Zhao, Baowei; US2010/29729; (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.1000343-13-4,5-Bromo-6-methyl-1H-indole,as a common compound, the synthetic route is as follows.

5-Bromo-1,6-dimethyl-1H-indole (FJG. 2, compound 2) was synthesized as follows. A flame-dried round-bottom flask was charged with compound 14 (5.41 g, 25.8 mmol, 1.0 eq., FJG. 2) and anhydrous THF (50 mL). The solution was cooled in an ice-bath and treated with NaH as a 60%dispersion in mineral oil (1.24 g, 30.9 mmol, 1.2 eq.) and methyl iodide (3.2 mL, 51.5 mmol, 2.0 eq.). After stirring at 0 C for 2 hrs, the volatiles were removed under reduced pressure. The residue was dissolved with CH2C12 (100 mL) and washed with brine (50 mL). The organic fraction was (Na2SO4), filtered and concentrated to afford the crude product which was purified via flash chromatography on a silica column (7:193 v/v EtOAc:Hexanes) to afford the title compound as a yellow solid (4.56 g, 20.3 mmol, 79.1% yield). ?H NMR (500 MHz, Acetone-d6) 10.27 (bs, NH), 7.82 (s, 1H), 7.41 (s, 1H), 7.31 (dd, J= 3.2, 2.4 Hz, 1H), 6.45 (td, J= 2.1, 1.0 Hz, 1H), 2.48 (d, J= 0.8 Hz, 3H). ?3C NMR (125 MHz, Acetone-d6) 136.1, 129.7, 128.5, 126.0, 123.5, 115.6, 113.2, 101.1, 23.1. m.p. = 90-91 C. JR (neat):33143118, 3095, 1467, 1338 1753, 1705, 1614, 1507, 1468, 1270, 993, 881, 842, 730, 693, 606 cm?. HR-MS calculated for C,0H,0BrN [M+H] m/z 224.0075, found 224.0079., 1000343-13-4

The synthetic route of 1000343-13-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; CHANG, Christopher J.; BREWER, Thomas Francis; CHAN, Jefferson; (109 pag.)WO2017/34927; (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.26807-73-8,1-Benzyl-1H-indol-5-amine,as a common compound, the synthetic route is as follows.

[Example 113] (1065) (1066) The mixture of 80 mg of 1-benzyl-1H-indol-5-amine, 100 mg of methyl 2-iodo-5-isopropylbenzoate, 15 mg of tris(dibenzylideneacetone)dipalladium(0), 19 mg of 4,5′-bis(diphenylphosphino)-9,9′-dimethylxanthene, 214 mg of cesium carbonate, and 2 mL of toluene, was heated at reflux for three hours and 10 minutes under a nitrogen atmosphere. The insoluble matter was filtered off and the solvent was distilled off under reduced pressure. The obtained residue was purified by silica gel column chromatography (gradient elution with hexane:ethyl acetate = 100:0-80:20) to give 122 mg of methyl 2-((1-benzyl-1H-indol-5-yl)amino)-5-isopropylbenzoate as a yellow oil. MS (ESI, m/z): 399 (N4+H)+., 26807-73-8

As the paragraph descriping shows that 26807-73-8 is playing an increasingly important role.

Reference£º
Patent; Toyama Chemical Co., Ltd.; FUJIFILM Corporation; TANAKA, Tadashi; KONISHI, Yoshitake; KUBO, Daisuke; FUJINO, Masataka; DOI, Issei; NAKAGAWA, Daisuke; MURAKAMI, Tatsuya; YAMAKAWA, Takayuki; EP2915804; (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

1075-35-0, 5-Chloro-2-methylindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

a. A mixture consisting of 100 gm (0.6 mol) of 5-chloro-2-methyl-indole, 100 gm (0.65 mol) of 4-piperidone monohydrate hydrochloride, 900 ml of glacial acetic acid and 450 ml of 4 N phosphoric acid was heated for 2 hours at 80C. Thereafter, the reaction mixture was cooled and then poured into a mixture of ice and ammonia, and the resulting mixture was extracted with ethyl acetate. The organic extract solution was washed with water, dried and evaporated, and the residue was recrystallized from methanol, yielding 108 gm (73% of theory) of 4-(5′-chloro-2′-methyl-3′-indolyl)-1,2,5,6-tetrahydropyridine, m.p. 208-210C., 1075-35-0

1075-35-0 5-Chloro-2-methylindole 70636, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Boehringer Ingelheim GmbH; US3980658; (1976); 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.117140-77-9,1H-Indole-2,5-dicarboxylic acid,as a common compound, the synthetic route is as follows.

117140-77-9, Example 34 1-Propyl-1H-indole-2,5-dicarboxylic acid 87 Sodium hydride (60% suspension, 125 mg, 5 mmol) was added to a stirred solution of 1H-indole-2,5-dicarboxylic acid (525 mg, 2 mmol) in dry DMF (10 mL) and maintained at ambient temperature for 1 hour. The reaction was cooled to 0 C. and then propyl bromide (0.275 mL, 3 mmol) was added. After 3 days the reaction was quenched by addition of 5% aqueous NH4Cl. The mixture was concentrated to dryness and then purified on a silica gel column using 5% EtOAc/toluene. The product was then dissolved in 30 mL ethanol and 10 mL of 2 M NaOH was added. The solution was heated at 55 C. for 2 days. The ethanol was removed in vacuo and the resulting aqueous solution was acidified with 0.01 M HCl to pH 3. The resulting precipitate was filtered and rinsed twice with water. The isolated product was dried by evaporation from absolute ethanol (3*) to give 340 mg (67%) of 87. 1H NMR (CDCl3): delta8.38 (s, 1H, H-4 indole), 7.87 (d, 1H, H-6 indole), 7.71 (d, 1 H, H-7 indole), 7.44 (d, 1 H, H-3 indole), 4.53 (m, 2H, Propyl), 1.7 (m, 2H, propyl), 0.81 (m, 3H, propyl) MS: 246 [M-H]

The synthetic route of 117140-77-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Dyatkina, Natalia B.; Shi, Dong-Fang; Roberts, Christopher Don; Velligan, Mark Douglas; Reinhard Liehr, Sebastian Johannes; Botyanszki, Janos; Zhang, Wentao; Khorlin, Alexander; Nelson, Peter Harold; Muchowski, Joseph Martin; US2003/212113; (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

10102-94-0, 5-Bromo-1-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: 5-Nitro-1H-indazole-3-carbohydrazide (8, 500 mg,2.26 mmol, 1.0 eq.) was dissolved in 3 cm3 glacial acetic acid. To this reaction mixture 2.26 mmol indole-3-aldehyde(1.0 eq.) was added and heated at 90 C for 6 h. Later the reaction mass was neutralized with a cold NaHCO3 solution, filtered, and recrystallized from ethanol to afford 10a., 10102-94-0

As the paragraph descriping shows that 10102-94-0 is playing an increasingly important role.

Reference£º
Article; Sreenivasulu, Reddymasu; Sujitha, Pombala; Jadav, Surender Singh; Ahsan, Mohamed Jawed; Kumar, C. Ganesh; Raju, Rudraraju Ramesh; Monatshefte fur Chemie; vol. 148; 2; (2017); p. 305 – 314;,
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