Day: August 25, 2020

348640-06-2, 4-Bromo-7-azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-bromo-lH-pyrrolo[2,3-b]pyridine (LXXIV) (5 g, 25.4 mmol, 1 eq.), DMAP (311 mg, 2.55 mmol, 0.1 eq.) and TEA (5.3 mL, 38 mmol, 3 eq.) in DCM (100 mL) was added B0C2O (7.2 mL, 31 mmol, 1.2 eq.) at 0C. The reaction was warmed to room temperature and stirred for 2 h. Water (100 mL) was added and extracted with DCM (x 2). Removal solvents gave fert-butyl 4-bromo-lH-pyrrolo[2,3-b]pyridine-l-carboxylate (LXXV) as a colorless oil (6.95 g, 23.4 mmol, 92.1% yield). NMR (CDCI3, 400 MHz) delta ppm 1.60 (s, 9H), 6.50 (d, J=4Hz, 1H), 7.31 (d, J=5.2Hz, 1H), 7.63 (d, J=4Hz, 1H), 8.23 (d, J=5.2Hz, 1H); ESIMS found for Ci2Hi3BrN202 mlz 297.1 (M+H).

348640-06-2 4-Bromo-7-azaindole 22273643, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; SAMUMED, LLC.; KC, Sunil Kumar; WALLACE, David Mark; CAO, Jianguo; CHIRUTA, Chandramouli; HOOD, John; (247 pag.)WO2017/24004; (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.24985-85-1,Ethyl 5-hydroxyindole-2-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of ethyl 5-hydroxy-1 H-indole-2-carboxylate (0.25g, 1 .22 mmol) in acetone (3ml_) was added K2C03 (0.51 g, 3.66 mmol) and cyclopropylmethyl bromide (.24ml_, 2.44 mmol). The mixture was heated to reflux overnight. After cooling, the mixture wasfiltered through celite and concentrated under reduced pressure. The crude product was purified using flash chromatography on silica gel with 8:2 hexanes/ethyl acetate as eluent to give 131 mg of the title compound.

The synthetic route of 24985-85-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARISAN THERAPEUTICS INC.; PLEWE, Micheal; WHITBY, Landon; MCCORMACK, Kenneth; HENKEL, Gregory; BROWN, Eric; BOGER, Dale; SOKOLOVA, Nadezda; REDDY, Vidyasagar; (319 pag.)WO2016/160677; (2016); 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.4382-54-1,5-Methoxyindole-2-carboxylic acid,as a common compound, the synthetic route is as follows.

General procedure: A mixture of 5-methoxyindole-2-carboxylic acid 1 (20 g, 104.61 mmol) and sulfuric acid (16 mL) in EtOH (160 mL) was refluxed for 10 h. The reaction mixture was evaporated, neutralized to pH 7 with 2 N-NaOH and extracted with ethyl acetate. The organic layer was dried over anhydrous Na2SO4, and evaporated under reduced pressure. The residue was purified by silica gel column chromatography using solvent CH2Cl2 and isolated by ether to give 5-methoxyindole-2-carboxylic acid ethyl ester (22.8 g, 99percent). Mp 157 ¡ãC; IR (ATR) vmax=3325, 1676 cm-1; Rf 0.39 (n-Hexane/EtOAc, 4:1); 1H NMR (300 MHz, CDCl3) delta 8.81 (br s, 1H), 7.31 (d, J=8.9 Hz, 1H), 7.16-7.05 (m, 2H), 7.00 (dd, J=9.0, 2.1 Hz), 4.40 (q, J=7.1 Hz, 2H), 3.85 (s, 3H), 1.41 (t, J=7.1 Hz, 3H). 13C NMR (75 MHz, CDCl3); delta 162.0, 154.7, 132.3, 127.9, 127.8, 116.7, 112.8, 108.2, 102.5, 60.9, 55.7, 14.4.

4382-54-1 5-Methoxyindole-2-carboxylic acid 20401, aindole-building-block compound, is more and more widely used in various.

Reference£º
Article; Pagire, Haushabhau S.; Chun, Hang-Suk; Bae, Myung Ae; Ahn, Jin Hee; Tetrahedron; vol. 69; 14; (2013); p. 3039 – 3044;,
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

32996-16-0, Ethyl 1H-indole-5-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A solution of the appropriate ethyl or methyl esters 21a-d (1.0 mmol) in methanol (5 mL) was prepared in a 10 mL CEM microwave vessel. Hydrazine hydrate 50% (5.0 mmol) was added, the vessel was capped and placed in a microwave reactor and the reaction carried out with the following method in dynamic mode: 140 C, 60 min, 100 W, with high stirring. After completion the reaction mixture was transferred to a round bottom flask and the solvent evaporated under reduced pressure. The crude product was transferred to an Erlenmeyer flask and suspended in dichloromethane, heated at 50 C for 5 min, rapidly vacuum filtered and washed with the same solvent, to obtain the pure product (yield 80-90%). When the product was found to be still not pure, the purification procedure was repeated.

32996-16-0 Ethyl 1H-indole-5-carboxylate 10987040, aindole-building-block compound, is more and more widely used in various.

Reference£º
Article; Rupiani, Sebastiano; Buonfiglio, Rosa; Manerba, Marcella; Di Ianni, Lorenza; Vettraino, Marina; Giacomini, Elisa; Masetti, Matteo; Falchi, Federico; Di Stefano, Giuseppina; Roberti, Marinella; Recanatini, Maurizio; European Journal of Medicinal Chemistry; vol. 101; (2015); 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.6245-89-2,(1H-Indol-3-yl)-1-propanamine,as a common compound, the synthetic route is as follows.

General procedure: The carboxylic acid (1.0?equiv) and the amine (1.0?1.1?equiv) were dissolved in CH2Cl2 (3?4?mL/mmol) and treated with N-(3-dimethylaminopropyl)-N?-ethylcarbodiimide hydrochloride (EDC) (1.1?equiv), 1-hydroxybenzotriazole hydrate (HOBt) (1.1?equiv), and Et3N (2.4?equiv or 3.4?equiv for amine hydrochlorides) and stirred at rt overnight. If the reaction was heterogeneous, DMF was added until homogeneity was obtained. The reaction mixture was washed with water, 10percent aq HCl solution, and satd aq NaHCO3 solution then dried over anhydrous sodium sulfate and concentrated under reduced pressure.

The synthetic route of 6245-89-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Goff, Dane A.; Tetrahedron; vol. 69; 1; (2013); p. 242 – 256;,
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

15317-58-5, 1H-Indole-3-carbohydrazide is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General Procedure: To a mixture of indole-3-carboxaldehyde 2 (1 mmol) and indole-3-carbohydrazide 4 (1 mmol) in ethanol(10 mL) was added catalytic amount of acetic acid (0.1 mL). The reaction mixture was refluxed for 3-4 h. Progress of the reaction was monitored by thin layer chromatography. Upon completion, the reaction mixture was cooled, and solid mass so obtained was filtered and recrystallized to afford pure bis(indolyl)hydrazide-hydrazones 5a-n in good yields.

15317-58-5 1H-Indole-3-carbohydrazide 27199, aindole-building-block compound, is more and more widely used in various.

Reference£º
Article; Kumar, Dalip; Maruthi Kumar; Ghosh, Soumitra; Shah, Kavita; Bioorganic and Medicinal Chemistry Letters; vol. 22; 1; (2012); p. 212 – 215;,
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

15317-58-5, 1H-Indole-3-carbohydrazide is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 1H-Indole-3-carboxylate methylester 2 (1.0 mmol-equiv.) was refluxed with hydrazine hydrate(12.5 g, 0.25 M) in appropriate ethanol (30 mL) for 2 h. The progressof the reaction was monitored by TLC. After cooling the reactionmixture to room temperature, the mixtures were filtered to givewhite solid crude products without purification. Next, indolehydrazide(3, 1.0 mmol) in ethanol (30 mL) was added dropwiseinto the appropriate aldehyde (1.5 mmol-equiv.) and a few drops ofpropionic acid; the mixture was stirred and refluxed for 2.5 h. Aftercooling, the precipitates were filtered and washed several times bymethanol to yield the crystal substances 4aeu.

15317-58-5 1H-Indole-3-carbohydrazide 27199, aindole-building-block compound, is more and more widely used in various.

Reference£º
Article; Ju, Zhiran; Su, Mingzhi; Hong, Jongki; La Kim, Eun; Moon, Hyung Ryong; Chung, Hae Young; Kim, Suhkmann; Jung, Jee H.; European Journal of Medicinal Chemistry; vol. 180; (2019); p. 86 – 98;,
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

184150-96-7, Methyl 2-methyl-1H-indole-6-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Methyl 3-isobutyryl-2-methylindole-6-carboxylate (142 mg) was prepared from methyl 2-methylindole-6-carboxylate (305 mg) and isobutyryl chloride (0.47 ml) in a similar manner to that of Preparation 1 (5). NMR (CDCl3, delta): 1.26 (6H, d, J=7 Hz), 2.81 (3H, s), 3.47 (1H, m), 3.93 (3H, s), 7.92 (1H, d, J=8 Hz), 8.09 (1H, s), 8.85 (1H, br s).

The synthetic route of 184150-96-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Cell Pathways, Inc.; US6358992; (2002); B1;,
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

103858-52-2, Ethyl 4-bromo-1H-indole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a degassed solution of compound 33 (1.00 g, 3.94 mmol) and tributyl-(1 -ethoxyvinyl)stannane (1.58 g, 4.37 mmol) in DMF (25 mL) under argon was addedbis(triphenylphosphine)palladium(II) dichlonde (0.100 g, 0.142 mmol). The reaction mixture was stirred at room temperature until TLC revealed completion of the reaction (approx. 7 days). The mixture was concentrated under reduced pressure and the residue partitioned between ethyl acetate and water. The organic layer was filtered through a plug of silica gel, dried over MgSO4,and concentrated under reduced pressure. The resulting black oil was dissolved in methanol (100 mL), treated with 5N hydrochloric acid (100 mL), and stirred at room temperature overnight. The mixture was concentrated and the residue dissolved in ethyl acetate. The solution was washed with water, dried over Na2SO4, and concentrated under reduced pressure. The crude product was purified by silica gel column chromatography to give 0.500 g (2.30 mmol, 58%) ofcompound 66.

The synthetic route of 103858-52-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AICURIS GMBH & CO. KG; DONALD, Alastair; URBAN, Andreas; BONSMANN, Susanne; WEGERT, Anita; GREMMEN, Christiaan; SPRINGER, Jasper; (376 pag.)WO2019/86141; (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.36193-65-4,1H-Indole-2-carbonitrile,as a common compound, the synthetic route is as follows.

General procedure: Cyanoindole 6 (40 mg, 0.256 mmol, 1 equiv.), Mn(OAc)3.2H2O (345 mg, 1.29 mmol, 5 equiv),and diethyl malonate (205 mg, 1.28 mmol, 5 equiv) were dissolved in aceticacid (10 mL) and heated to reflux for 2 h. After TLC indicated complete consumption of the starting indole, the reaction was poured into water (200 mL) and extracted with ethyl acetate (3 50 mL). The combined organic extracts were washed with water (3 100 mL), brine (1 100 mL), dried over sodium sulfate, filtered, and concentrated in vacuo to give a brown oil. The product was purified via flash chromatography (silica gel, hexanes:EtOAc 4:1)to afford 15 as a white solid (90%);20

36193-65-4 1H-Indole-2-carbonitrile 3787599, aindole-building-block compound, is more and more widely used in various.

Reference£º
Article; Lopchuk, Justin M.; Montgomery, William L.; Jasinski, Jerry P.; Gorjifard, Sayeh; Gribble, Gordon W.; Tetrahedron Letters; vol. 54; 45; (2013); p. 6142 – 6145;,
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