Day: October 19, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1196-69-6,Indole-5-carboxaldehyde,as a common compound, the synthetic route is as follows.

To a solution of indole-3-carboxaldehyde (16, 28.5 g, 100 mmol) in ethanol (500 mL) at room temperature was added potassium hydroxide (6.2 g, 110 mmol); the mixture was stirred until total solubilization. The ethanol was completely removed in a vacuum and acetone (250 mL) was added followed by benzenesulfonyl chloride (19.4 g, 110 mmol). The precipitate was filtered off, and the filtrate was concentrated and recrystallized from methanol to give a white solid. Yield: 40%., 1196-69-6

As the paragraph descriping shows that 1196-69-6 is playing an increasingly important role.

Reference£º
Article; Chen, Jianjun; Li, Chien-Ming; Wang, Jin; Ahn, Sunjoo; Wang, Zhao; Lu, Yan; Dalton, James T.; Miller, Duane D.; Li, Wei; Bioorganic and Medicinal Chemistry; vol. 19; 16; (2011); p. 4782 – 4795;,
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.703-80-0,3-Acetylindole,as a common compound, the synthetic route is as follows.

703-80-0, To a solution of 3-acetylindole 8a (1.0 g, 6.3 mmol) in THF (5.0 mL) sodium hydride (60% dispersion in mineral oil, 0.3 g, 6.3 mmol) was added at 0 C and the mixture was stirred at room temperature for 1 h. p-toluenesulfonyl chloride (1.2 g, 6.3 mmol) was added and the mixture was stirred at room temperature for 24 h. The residue was evaporated under reduced pressure, treated with water (20 mL) and extracted with EtOAc (3 ¡Á 20 mL). The organic phase was dried (Na2SO4), evaporated under reduced pressure and purified by column chromatography using DCM as eluent. White solid; yield: 90%; mp: 148-149 C; IR 1662 (CO), 1382, 1299 (SO2) cm-1; 1H NMR (200 MHz, DMSO-d6) delta: 2.33 (s, 3H, CH3), 2.60 (s, 3H, CH3), 7.32-7.39 (m, 2H, H-5, H-6), 7.43 (d, 2H, J = 7.8 Hz, H-3?, H-5?), 7.95 (d, 1H, J = 7.5 Hz, H-7), 8.04 (d, 2H, J = 7.8 Hz, H-2?, H-6?), 8.19 (d, 1H, J = 7.5 Hz, H-4), 8.81 (s, 1H, H-2); 13C NMR (50 MHz, DMSO-d6) delta:21.0 (q), 27.8 (q), 113.0 (d), 120.7 (s), 122.3 (d), 124.8 (d), 125.6 (d), 127.0 (s), 127.2 (2xd), 130.5 (2xd), 133.5 (s), 134.0 (s), 134.2 (d), 146.2 (s), 193.9 (s). Anal. Calcd for: C17H15NO3S: C, 65.16; H, 4.82; N, 4.47. Found: C, 65.28, H, 5.06, N, 4.37.

703-80-0 3-Acetylindole 12802, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Parrino, Barbara; Carbone, Anna; Di Vita, Gloria; Ciancimino, Cristina; Attanzio, Alessandro; Spano, Virginia; Montalbano, Alessandra; Barraja, Paola; Tesoriere, Luisa; Livrea, Maria Antonia; Diana, Patrizia; Cirrincione, Girolamo; Marine Drugs; vol. 13; 4; (2015); p. 1901 – 1924;,
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.120-72-9,1H-Indole,as a common compound, the synthetic route is as follows.

Dimethylsulfoxide (2 mL) was added to a 25 mL pressure-resistant reaction tube, indole (35.1 mg, 0.3 mmol), ethyl trifluoropyruvate(102.0 mg, 0.6 mmol), Cuprous chloride (44.78 mg, 1.5 eq.), The reaction was magnetically stirred in an 80 C oil bath for 12 hours. After the reaction was completed, most of the solvent was distilled off under reduced pressure, and the remaining mixture was purified by column chromatography on petroleum ether / ethyl acetate (10: 1) as eluent to obtain the desired product, As a pale yellow solid, 35.8 mg, yield 56%, 120-72-9

The synthetic route of 120-72-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Lishui College; Yan Guobing; Huang Dayun; He Ping; Cao Xihan; Zheng Wanbin; Ke Qiumin; Shen Xuqian; (5 pag.)CN106946758; (2017); 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

16066-91-4, 5-Iodo-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The reaction was performed in high pressure autoclave of 100 mL capacity manufactured by M/s Amar Industries. Toluene (10 mL), Pd(acac)2 (3 mg, 1 mol %), and dppm (7.7 mg, 2 mol %) were added to the autoclave reactor. To this solution iodobenzene (204 mg, 1.0 mmol), n-hexadecane (50 mg, internal GC standard), TMEDA (N,N,N’,N’-tetramethylethylenediamine, 1 equiv) were added. The mixture was flushed twice with CO/H2 1:1, then synthetic gas pressure was adjusted to 10 bar and the mixture was heated at 100 C for 10 h. After completion of reaction, the reaction mixture was cooled to room temperature. The light yellow colored solution was evaporated and residue obtained was purified by column chromatography (silica gel, mesh size 60-120) using pet ether/ethyl acetate (95:05) as eluent to get the desired formylated product., 16066-91-4

The synthetic route of 16066-91-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Singh, Abhilash S.; Bhanage, Bhalchandra M.; Nagarkar, Jayashree M.; Tetrahedron Letters; vol. 52; 18; (2011); p. 2383 – 2386;,
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

84807-09-0, 4-(Piperazin-1-yl)-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,84807-09-0

EXAMPLE 12 1-[N-(2-nitrophenyl)-2-aminoethyl]-4-(4-indolyl)piperazine A mixture containing 0.49 g of N-(2-chloroethyl)-2-nitroaniline, prepared according to the procedure described by Ramage G. R. et al. in J. Chem. Soc. 4406-4409 (1952), 0.55 g of 1-(4-indolyl)piperazine (prepared according to WO 95/33743), 1 mL of triethylamine and 3 mL of DMF was heated at reflux while stirring under nitrogen for 2.5 h. After cooling at room temperature, the mixture was poured into H2 O, extracted with CH2 Cl2, and the organic phase dried on anhydrous Na2 SO4 and evaporated to dryness. The residue was purified via flash chromatography (EtOAc-petrolium ether 3:7) giving 0.35 g (40percent) of the title compound. 1 H-NMR (CDCl3, delta): 8.60-8.45 (br, 1H, aniline NH), 8.18 (dd, 1H, aniline H3), 8.20-8.10 (br, 1H, indole NH), 7.43 (td, 1H, aniline H5), 7.20-7.05 (m, 3H, indole H3,6,7), 6.85 (dd, 1H, aniline H4), 6.70-6.57 (m, 2H, aniline H6 and indole H5), 6.50 (t, 1H, indole H2), 3.45 (q, 2H, NHCH2 CH2), 3.35-3.25 (m, 4H, piperazine protons), 3.85-2.70 (m, 6H, NHCH2 CH2 and piperazine protons).

The synthetic route of 84807-09-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Recordati S.A. Chemical and Pharmaceutical Company; US6071920; (2000); 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.169674-02-6,4-Chloro-5-fluoro-1H-indole,as a common compound, the synthetic route is as follows.

4-chloro-5-fluoro-1 H-pyrrolo[2,3-b]pyridine (500 mg, 2.931 mmol) in dioxane (12 ml.) was warmed to 40 C until a solution resulted. 4M HCI in dioxane solution (800 muIota_, 3.224 mmol) was added dropwise. The reaction mixture was cooled to room temperature and filtered. The solid was washed with diethyl ether and dried. It was then suspended in acetonitrile (10 ml.) and treated with sodium iodide (2.63 g, 17.55 mmol). The reaction mixture was heated at 80 C overnight. After cooling to room temperature, reaction mixture was treated with 1 N sodium hydroxide solution until it was basic. It was then extracted with ethyl acetate and washed with water. The combined organic layers were washed with saturated aqueous sodium chloride solution, dried, filtered and concentrated under reduced pressure to afford 5-fluoro-4-iodo-1 H-indole., 169674-02-6

169674-02-6 4-Chloro-5-fluoro-1H-indole 11607987, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; GILEAD SCIENCES, INC.; DU, Zhimin; GUERRERO, Juan, Arnaldo; KAPLAN, Joshua, Aaron; KNOX, JR., John Edward; NADUTHAMBI, Devan; PHILLIPS, Barton, W.; VENKATARAMANI, Chandrasekar; WANG, Peiyuan; WATKINS, William, J.; ZABLOCKI, Jeff; WO2015/187684; (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

942-26-7, 5-Chlorotryptamine hydrochloride is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

942-26-7, Triethylamine (1.93 mL; 13.78 mmol) was added at 0 C. to a mixture of 2-(5-chloro-1H-indol-3-yl)ethanamine hydrochloride (1.3 g; 5.51 mmol) and 3-(chloromethyl)benzoyl chloride (1.13 g; 5.79 mmol) in dichloromethane (75 mL). The mixture was stirred for 20 minutes at room temperature and was evaporated to dryness. The residue was purified by flash chromatography on silica gel (eluent 2 to 20% ethyl acetate in dichloromethane) to furnish 1.45 g (76%) of N-(2-(5-chloro-1H-indol-3-yl)ethyl)-3-(chloromethyl)benzamide as a white solid. [0561] ESI/APCI(+): 347 (M+H), 369 (M+Na); ESI/APCI(-): 345 (M-H). [0562] 1H NMR (DMSO-d6) delta 11.04 (s, 1H); 8.68 (t, 1H); 7.91 (s, 1H); 7.80 (d, 1H); 7.63 (s, 1H); 7.59 (d, 1H); 7.47 (t, 1H); 7.35 (d, 1H); 7.28 (s, 1H); 7.06 (dd, 1H); 4.82 (s, 2H); 3.52 (q, 2H), 2.93 (t, 2H).

As the paragraph descriping shows that 942-26-7 is playing an increasingly important role.

Reference£º
Patent; Griffioen, Gerard; Van Dooren, Tom; Rojas De La Parra, Veronica; Allasia, Sara; Marchand, Arnaud; Kilonda, Amuri; Chaltin, Patrick; US2013/274260; (2013); 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

942-26-7,942-26-7, 5-Chlorotryptamine hydrochloride is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A flask was charged with 5-chlorotryptamine hydrochloride (5 g, 0.0649 mol), 0.5 M hydrochloric acid(130 mL), and the substituted benzaldehyde (1.5 eq). The mixture was refluxed for 14 hr, cooled to roomtemperature, and vacuum filtered. The solid was resuspended in acetic acid (100 mL), stirred for 1 hr, andvacuum filtered. The solid was resuspended in ethyl acetate (100 mL), stirred for 1 hr, and vacuumfiltered to obtain the pure scaffold as a solid.

942-26-7 5-Chlorotryptamine hydrochloride 2827494, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Tikhmyanova, Nadezhda; Paparoidamis, Nicholas; Romero-Masters; Feng, Xin; Mohammed, Farheen Sultana; Reddy, Poli Adi Narayana; Kenney, Shannon C.; Lieberman, Paul M.; Salvino, Joseph M.; Bioorganic and Medicinal Chemistry Letters; vol. 29; 16; (2019); p. 2259 – 2264;,
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

244-69-9, 5H-Pyrido[4,3-b]indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A solution of 4 mmol carboline (12 or 14) and 4.4 mmol of NaH in DMF was stirred at room temperature for 30 min. After addition of 4.4 mmol of corresponding alkyl halide the solution was stirred for another 4-16 h. The conversion was monitored by TLC and GC/MS. When no further reaction was observed the solution was poured into iced water extracted with dichloromethane and purified by column chromatography and was subsequently converted into its HCl salt in 2-propanol with ethereal HCl., 244-69-9

Big data shows that 244-69-9 is playing an increasingly important role.

Reference£º
Article; Otto, Robert; Penzis, Robert; Gaube, Friedemann; Winckler, Thomas; Appenroth, Dorothea; Fleck, Christian; Traenkle, Christian; Lehmann, Jochen; Enzensperger, Christoph; European Journal of Medicinal Chemistry; vol. 87; (2014); p. 63 – 70;,
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.14805-29-9,exo-Hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione,as a common compound, the synthetic route is as follows.

A mixture of bicyclo[2.2.1]heptane-2,3-di-exo-carboximide (prepared as described in Chem. Pharm. Bull., 1991 p 2288; 1.0 g, 6.05 mmol), ethyl chloroacetate (1.3 mL, 12.1 mmol), TBAB (39 mg, 0.12 mmol) and potassium carbonate (1.17 g, 8.48 mmol) were irradiated in microwawe for 10 min at 150 C. (150 W). The mixture was then diluted with water and EtOAc. Organic phase was separated, and aqueous phase was extracted with EtOAc (3¡Á15 mL). Combined organic phases were washed with brine (1¡Á15 mL), dried over Na2SO4, filtered and concentrated to afford the title compound as a brown oil (1.74 g, 114%)., 14805-29-9

As the paragraph descriping shows that 14805-29-9 is playing an increasingly important role.

Reference£º
Patent; Merck Patent GmbH; JORAND-LEBRUN, Catherine; JOHNSON, Theresa L.; GRAEDLER, Ulrich; JIANG, Xuliang; KULKARNI, Santosh; (23 pag.)US2017/283427; (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