Indole Building Blocks

4769-96-4,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4769-96-4,6-Nitro-1H-indole,as a common compound, the synthetic route is as follows.

To a solution of 6-nitro indole (1 eq.) in a mixture of acetic acid(0.15 M) and hydrochloric acid (0.6 M), SnCl2 (10 eq.) was added.The reaction mixture proceeded and 1H NMR was recorded, aspreviously reported

4769-96-4 6-Nitro-1H-indole 78502, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Hendy, Moataz S.; Ali, Aya A.; Ahmed, Lubna; Hossam, Reham; Mostafa, Alaa; Elmazar, Mohamed M.; Naguib, Bassem H.; Attia, Yasmeen M.; Ahmed, Mahmoud Salama; European Journal of Medicinal Chemistry; vol. 166; (2019); p. 281 – 290;,
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

90858-86-9, 4-Bromo-5-methoxy-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

90858-86-9, Synthesis of 3-(5-Methoxy-1H-Indol-4-yl)-3-phenyl-acrylic acid ethyl ester (XLVIII) A mixture of 4-bromo-5-methoxyindole XLVI (104 mg, 0.46 mmol), ethyl cinammate (162 mg, 0.92 mmol), tetra-butylammonium bromide (29.6 mg, 0.092 mmol), TEA (128 mul, 0.092 mmol) and palladium-dichloro-[bis(tri-ortho-tolyl)phophine] (18 mg, 0.023 mmol) in DMF (2 ml) was stirred at 110¡ã C. for 3 hours. The reaction mixture was cooled to room temperature and partitioned between brine and EtOAc. The organic layers were combined, dried over Na2SO4, filtered, concentrated, and purified via flash chromatography (hexane/EtOAc) affording 3-(5-Methoxy-1H-Indol-4-yl)-3-phenyl-acrylic acid ethyl ester XLVIII (37 mg, impure).

As the paragraph descriping shows that 90858-86-9 is playing an increasingly important role.

Reference£º
Patent; Roche Palo Alto LLC; US2007/123527; (2007); 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.16502-01-5,2,3,4,9-Tetrahydro-1H-pyrido[3,4-b]indole,as a common compound, the synthetic route is as follows.

To a stirred solution of tryptoline (2,3,4,9-tetrahydro-1 /-/-pyrido[4,3-b]indole) (150 g, 0.871 mol) in THF (1 .5 L) at 0 C, triethylamine (243 ml_, 1 .74 mol) and di-ferf-butyl dicarbonate (228 g, 1.04 mol) were added and the reaction mixture was stirred at 25 C for 12 h. After the completion of the reaction (monitored by TLC), water was added to the reaction mixture under ice-cooling and extracted with ethyl acetate (2 x 500 ml_). The combined organic extracts were washed with brine (1 x 250 ml_), dried over anhydrous Na2S04,filtered and evaporated under reduced pressure to get the crude product. The crude material was stirred with diethyl ether (200 mL) and the solid thus obtained was filtered, washed with diethyl ether (2 x 100 mL) and dried to afford the title compound as brown solid (200 g, 84 %).1H-NMR (400 MHz, CDCI3) d = 7.94 (br-s, 1 H), 7.51 (d, J = 7.60 Hz, 1 H), 7.33-7.34 (m, 1 H), 7.1 1 -7.13 (m, 2H), 4.67 (s, 2H), 3.79 (br-s, 2H), 2.83 (br-s, 2H), 1.53 (s, 9H).MS: 273.2 (M+H)+., 16502-01-5

16502-01-5 2,3,4,9-Tetrahydro-1H-pyrido[3,4-b]indole 107838, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; AC IMMUNE SA; NAMPALLY, Sreenivasachary; GABELLIERI, Emanuele; MOLETTE, Jerome; (0 pag.)WO2019/233883; (2019); 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

107516-75-6, Diethyl 1H-indole-2,6-dicarboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 2: Synthesis of diethyl l-{3-[(tert-butoxycarbonyl)amino]-2,2-dimethylpropyl}- 1H-indole-2,6-dicarboxylate To a solution of diethyl 1H-indole-2,6-dicarboxylate (25.3 g, 97 mmol), tert-butyl (3- hydroxy-2,2-dimethylpropyl)carbamate (19.7, 97 mmol) and triphenylphosphine (50.9 g, 194 mmol) in THF (200 mL) is added and diisopropyl azodicarboxylate (40.2 mL, 194 mmol). The mixture is stirred for 60 h at room temperature and then the solvent is removed. The residue is separated into two portions and each of them is filtered through a short plug of silica gel (400 g) using 20% EtOAc in heptane. A mixture of diethyl l-{3- [(tert-butoxycarbonyl)amino]-2,2-dimethylpropyl}-1H-indole-2,6-dicarboxylate and diethyl 1H-indole-2,6-dicarboxylate (55 g) is obtained and the mixture is used in the next step without further purification.

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 INTERNATIONAL GMBH; BOYER, Stephen, James; GAO, Donghong, Amy; GUO, Xin; KIRRANE, Thomas, Martin, Jr.; SARKO, Christopher, Ronald; SNOW, Roger, John; SOLEYMANZADEH, Fariba; ZHANG, Yunlong; WO2011/71716; (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.52562-50-2,5-Methyl-1H-indole-3-carbaldehyde,as a common compound, the synthetic route is as follows.

52562-50-2, General procedure: An equimolar mixture of Gewald adducts (5CN, 6CN, 7CN and 8CN) and substituted indole-carboxaldehydes in absolute ethanol with 0.5 mL of acetic acid was stirred under room temperature for 24 hs. Water was addedand the solid that precipitated out was filtered under vacuum, washed with water, dried and recrystallized from absolute ethanol (Scheme 1) according previously methodology [20].

As the paragraph descriping shows that 52562-50-2 is playing an increasingly important role.

Reference£º
Article; Felix, Mayara B.; de Souza, Edson R.; de Lima, Maria do C.A.; Frade, Daiana Karla G.; Serafim, Vanessa de L.; Rodrigues, Klinger Antonio da F.; Neris, Patricia Lima do N.; Ribeiro, Frederico F.; Scotti, Luciana; Scotti, Marcus T.; de Aquino, Thiago M.; Mendonca Junior, Francisco Jaime B.; de Oliveira, Marcia R.; Bioorganic and Medicinal Chemistry; vol. 24; 18; (2016); p. 3972 – 3977;,
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

942-24-5, Methyl indole-3-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Hydrazine hydrate (99%, 2 mL, 40 mmol) was added in one portion to methyl indole-3-carboxylate 1 (10 mmol, 1.75 g) dissolved in dry ethanol (50 mL) at room temperature, and the resulting solution was heated under reflux for 8 h. The reaction mixture was allowed to cool and the solid obtained was filtered off and washed with a small quantity of ethanol to give the 1H-indole-3-carbohydrazide 2. Yield: 1.66 g, 95%, white solid, mp 234-236C; 1H NMR (600 MHz, DMSO-d6): delta 4.34 (s, 2H), 7.10-7.11 (m, 2H), 7.43 (t, J 3.6 Hz, 2H), 7.98 (s, 1H), 8.15 (d, J 7.2 Hz, 3H), 9.18 (s, 1H),11.55 (s,1H); EI-MS:m/z (%) 175 (M, 22),144 (100),116 (17), 89 (11)., 942-24-5

The synthetic route of 942-24-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Zhang, Ming-Zhi; Mulholland, Nick; Beattie, David; Irwin, Dianne; Gu, Yu-Cheng; Chen, Qiong; Yang, Guang-Fu; Clough, John; European Journal of Medicinal Chemistry; vol. 63; (2013); p. 22 – 32;,
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.5192-23-4,4-Aminoindole,as a common compound, the synthetic route is as follows.

General procedure: The solution of isatin (380 mumol), 1H-indole-4-amine (380 mumol, 1.0 equiv), and Meldrum’s acid (380 mumol, 1.0 equiv) in DMF (4.0 ml) was heated to 120 C for 2 h. The reaction mixture was cooled down to room temperature and concentrated to remove the solvents. The crude residue was subjected to reverse phase preparative HPLC to provide pure products., 5192-23-4

As the paragraph descriping shows that 5192-23-4 is playing an increasingly important role.

Reference£º
Article; Zou, Bin; Chen, Chun; Leong, Seh Yong; Ding, Mei; Smith, Paul W.; Tetrahedron; vol. 70; 3; (2014); p. 578 – 582;,
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

The title compound of this step was prepared by the method described in Example 1, Step 3, namely, 5 -(2-(piperazin- 1 -yl)pyrimidin-5 -yl)pyridine-2-carboxamide dihydrochloride (400 mg, 1.12 mmol), 3-(4-chlorobutyl)-1H-indole-5-nitrile (312 mg, 1.34 mmol), anhydrous sodium carbonate (712 mg, 6.72 mmol) and sodium iodide (50 mg, 0.33 mmol) were added to anhydrous acetonitrile (15 mL). The mixture solution was heated to 90 C and reacted for 36 hours. The crude product was separated and purified by column chromatography (dichloromethane/methanol (v/v) = 20/1) to give the title compound as a white solid (390 mg, 73.6%).MS (ESI, pos. ion) m/z: 481.70 [M+H].?H N?1R (600 IVIHz, DMSO-c16) (ppm): 11.36 (s, 1H), 8.92 (s, 1H), 8.83 (s, 2H),8.318.18 (m, 1H), 8.07 (d, J= 10.5 Hz, 3H), 7.63 (s, 1H), 7.50 (d, J 8.4 Hz, 1H), 7.40 (d, J8.4 Hz, 1H), 7.34 (s, 1H), 3.80 (brs, 4H), 2.74 (t, J= 7.3 Hz, 2H), 2.42 (brs, 4H), 2.37 (t, J 7.0Hz, 2H), 1.67 (dd, J= 14.6, 7.4 Hz, 2H), 1.54 (d, J= 6.6 Hz, 2H); HPLC: 99.42%., 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; SUNSHINE LAKE PHARMA CO., LTD.; JIN, Chuanfei; ZHONG, Wenhe; LIANG, Haiping; ZHANG, Yingjun; (79 pag.)WO2019/62662; (2019); 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.169674-01-5,5,6-Difluoroindole,as a common compound, the synthetic route is as follows.,169674-01-5

Trifluoroacetic anhydride (38 mL, 56.0 g, 0.27 mol) was added dropwise to a solution of 5,6-difluoro-lH-indole (0.22 mol) in DMF (300 mL) over 0.5 h at 0C. The reaction mixture was allowed to warm to room temperature and stirred overnight. The mixture was quenched with water (1 L), many solid began to form, the mixture was stirred for 0.5 h, then filtered. The solid was collected, washed with water (200 mL><3), then added to aqueous sodium hydroxide (20%, 150 mL, 0.75 mol) and heated under reflux for 8 h. The reaction mixture was cooled and acidified with aqueous 3N HC1 to pH of 3. Many solid began to form. The solid was collected by filter, washed with water (200 mL><3), dried to give title compound 91-1 (15.53 g, 59% yield). 169674-01-5 5,6-Difluoroindole 2778732, aindole-building-block compound, is more and more widely used in various fields. Reference£º
Patent; ARIAGEN, INC.; COLABUONO, Peter; JOHNSON, Graham; MANNING, David Douglas; WOLF, Mark Allan; (312 pag.)WO2019/99977; (2019); 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.15861-24-2,Indole-5-carbonitrile,as a common compound, the synthetic route is as follows.

General procedure: Typical procedure for the Friedel-Crafts reaction of indoles to alpha,beta-unsaturated ketones: To a stirred mixture of indole (117 mg, 1mmol), and methyl vinyl ketone (85 mg, 1.2 mmol) in H2O/THF (7:3, 2 mL ) solution, GO (20 mg) was added. The reaction mixture was allowed to stir at room temparature and progress of the reaction was monitored by TLC. After complete consumption of indole, water (5 mL) was added and the aqueous layer was extracted with ethyl acetate (2 X 5 mL). The combined organic extracts were dried with anhydrous Na2SO4. The solvent and volatiles were completely removed under vacuum to give the crude product, which was passed through a short pad of silica gel (petroleum ether/ethyl acetate) to afford the analytically pure product in 94% yield.The aqueous layer containing the catalyst was filtered and washed with acetone,water and dried in a dessicator and used for the next cyle., 15861-24-2

The synthetic route of 15861-24-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Vijay Kumar; Rama Rao; Tetrahedron Letters; vol. 52; 40; (2011); p. 5188 – 5191;,
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