Day: October 22, 2020

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.,35320-67-3

To a stirred solution of 2-chloro-N-[(3- fluorophenyl)methyl]-6,7-dihydro-5H-pyrano[2,3-d]pyrimidin-4-amine (7 g, 23.83 mmol) in anhydrous dioxane (140 mL) were added 2-methyl-1H-indol-4- ol (3.5 g, 23.83 mmol), Pd2dba3 (2.9 g, 2.38 mmol), X-Phos (2.3 g, 4.77 mmol) and Cs2CO3 (15.5 g, 47.66 mmol). The suspension was refluxed under N2 for 2 h. LCMS showed the reaction was completed. The mixture was filtered through a pad of celite, and the filter cake was washed with EtOAc (200 mL x 2). The organics were combined and concentrated in vacuo. The red residue was solidified by MTBE and EtOAc (100 mL/20 mL), the solid was collected by filtration and dried in vacuo to afford the product (7.5 g, 77%) as a brown solid. The filtrate was concentrated in vacuo and purified by silica gel column (hexane and ethyl acetate) to afford the 2nd fraction product (1.5 g) as a brown solid. LCMS (M+H+) m/z: Calcd: 405.1; Found: 405.1.

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; CLEAVE BIOSCIENCES, INC.; ZHOU, Han-Jie; WUSTROW, David; (498 pag.)WO2016/200840; (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.15903-94-3,6-(Benzyloxy)-1H-indole,as a common compound, the synthetic route is as follows.

General procedure: A test tube containing 7-nitro-3-phenyl-2H-benzo[b][1,4]oxazin-2-one (0.1 mmol), indole (0.1 mmol) and chiral phosphoric acid (8.7 mg, 0.01 mmol) was added 1.0 mL acetone, then the mixture was stirred at room temperature until the reaction was complete (monitored by TLC). Finally, the reaction mixture was directly poured to the column chromatograpy, using petroleum ether:ether acetate (5:1) as eluent to afford product., 15903-94-3

As the paragraph descriping shows that 15903-94-3 is playing an increasingly important role.

Reference£º
Article; Zhao, Yunlong; Wang, Longsheng; Zhao, Junling; Tetrahedron Letters; vol. 58; 3; (2017); p. 213 – 217;,
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

1092114-59-4, 3-Iodo-1H-indole-5-carbonitrile is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of compound 69b: 3-iodo-l-tosyl-l/7-indole-5-carbonitrileTo a solution of 3-iodo-l//-indole-5-carbonitrile (2 g, 7.40 mmol) in DMF (20 mL) was added 60% NaH (538 mg, 22.38 mmol) portion wise at 0 C and the reaction was stirred for 10 min RT. To the above mixture at 0 C, p-TsCl (2.2 g, 11.19 mmol) solution in DMF (4 mL) was added and stirred for further 2 h at RT. The reaction was quenched with ice cold H20 (20 mL). The resulting suspension was filtered and the solid was washed with H20 (10 mL) and dried. The crude was purified with silica gel chromatography (eluent: 20% EtOAc in petroleum ether) to afford 3-iodo-l-tosyl-l//-indole-5-carbonitrile (3.0 g, 95.5%) as an off brown solid. .H NMR (400MHz, DMSO-d6): delta 8.30 (s, 1H), 8.13 (d, J=8.8Hz, 1H), 7.98 (d, J=8.4Hz, 2H), 7.87-7.81 (m, 2H), 7.43 (d, J=8.0Hz, 2H), 2.32 (s, 3H).

1092114-59-4, As the paragraph descriping shows that 1092114-59-4 is playing an increasingly important role.

Reference£º
Patent; AMGEN INC.; WANG, Hui-Ling; CEE, Victor, C.; HERBERICH, Bradley, J.; JACKSON, Claire, L., M.; LANMAN, Brian, Alan; NIXEY, Thomas; PETTUS, Liping, H.; REED, Anthony, B.; WU, Bin; WURZ, Ryan; TASKER, Andrew; WO2012/129338; (2012); 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.1477-49-2,3-Indoleglyoxylic Acid,as a common compound, the synthetic route is as follows.

1477-49-2, General procedure: To a solution of carboxylic acid (2.05 equiv.), diamine (1 equiv.), and PyBOP (2.05 equiv.) in DMF (1 mL) was added Et3N (3 equiv.). The reaction mixture was allowed to stir under N2 at room temperature for 23 h. The solution was dried in vacuo and the crude reaction product purified by C8 reversed-phase column chromatography (20%-30% MeOH/H2O (+0.05%TFA)) to afford the target diamide as the bis-trifluoroacetate salt or by silica gel column chromatography (0%-1% MeOH in CH2Cl2) to afford the target diamide as the free base.

The synthetic route of 1477-49-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Wang, Jiayi; Kaiser, Marcel; Copp, Brent R.; Marine Drugs; vol. 12; 6; (2014); p. 3138 – 3160;,
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

5416-80-8, 2-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: To a suspension of 2-methylindole-3-carboxaldehyde (7a) (200 mg, 1.26 mmol) and Cs2CO3 (1.34 g, 3.80 mmol) in N,N-dimethylformamide (4 mL) was added 2-fluorobenzaldehyde (210 muL, 1.99 mmol) under a nitrogen atmosphere. The reaction mixture was heated at 140 C until the indole substrate was all consumed (monitored by TLC), and then allowed to cool down to room temperature. The resulting mixture was filtered and washed with ethyl acetate (80 mL). The filtrate was washed with water (3 X 80 mL). The organic layer was dried over Na2SO4 and concentrated under reduced pressure. The residue was purified by flash column chromatography on silica gel (EtOAc/hexanes = 1:3) to afford the desired indolo[1,2-a]quinoline.

5416-80-8, The synthetic route of 5416-80-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Thanetchaiyakup, Adisak; Rattanarat, Hassayaporn; Chuanopparat, Nutthawat; Ngernmeesri, Paiboon; Tetrahedron Letters; vol. 59; 11; (2018); p. 1014 – 1018;,
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.

the mixture of the cyclic imine 3,4-dihydroisoquinoline (66 mg, 0.50 mmol);6,7-dihydrothieno[3,2-c]pyridine (51 mg, 0.38 mmol); 3,4-dihydro–carboline (63 mg, 0.38 mmol) or4,5-dihydro-3H-benz[c]azepine (55.3 mg, 0.38 mmol); and the electron-rich aromatic compound (7-, 6-,4-, or 5-azaindole (30 mg, 0.25 mmol)) were placed in a 10 mL pressurized reaction vial and heated ina microwave reactor, under the conditions given in Tables 1-3. In the case of 5-azaindole, 10 mol % ofp-TSA (4.3 mg, 0.025 mmol) as a catalyst was also added., 272-49-1

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

Reference£º
Article; Belasri, Khadija; Fueloep, Ferenc; Szatmari, Istvan; Molecules; vol. 24; 19; (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.26340-49-8,2-Iodo-1H-indole,as a common compound, the synthetic route is as follows.

26340-49-8, To dry is added into the reactor 1, 3, 5, 7 – four (3, 5 – diiodosalicylic -4 – octoxy) phenyl nitrogen mixed fluorine boron glimmer (403.4 mg, 0 . 20 mmol), 3 – (2 – iodo) indole (145.8 mg, 0 . 60 mmol), copper acetate (109.0 mg, 0 . 60 mmol), 2, 2 – bipyridyl (15.6 mg, 50 mol %), tetrabutyl ammonium fluoride (104.6 mg, 0 . 40 mmol), 1, 2 – dichloroethane (0.5 ml), acetonitrile (0.5 ml), under the protection of nitrogen, in the 120 C reaction under the condition of 2 hours. Cooling to room temperature after the completion of reaction, adding 10 ml dichloromethane dilution, then diatomite filter in combination with 10 – 20 ml of dichloromethane washing, removal of the solvent under reduced pressure, the residue by silica gel column chromatography (eluant: gradient elution: ethyl acetate/petroleum ether/dichloromethane=1/10/1 – 1/6/1, v/v) separation and purification, after vacuum drying to have a metallic luster of the brown solid target product R1 For 4 – dimethylamino, R2 For the 5 – cyano, R3 For the 5, 7 – dimethyl -7 carboxyl substituted indole target product 274.9 mg, yield 55%.

As the paragraph descriping shows that 26340-49-8 is playing an increasingly important role.

Reference£º
Patent; Sichuan University; Wu Di; Jiang Ruyong; You Jingsong; (10 pag.)CN107189488; (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

830-96-6, 3-Indolepropionic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: H2SO4 (98%) (0.5mL) was added to a stirred solution of raw material1 in CH3OH (10mL) at room temperature and the mixture was then stirred for 2-3 h at 80 C. TLC was used to monitor the reaction progress until it was complete. A large amount of ice water was then added to the mixture. A saturated solution of sodium carbonate was used to neutralise the mixture until white solid appeared. After filtering the mixed solution, compounds 2a-h (yield 91-99) were obtained., 830-96-6

The synthetic route of 830-96-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Ye, Ying; Suo, Yourui; Yang, Fang; Yang, Yongjing; Han, Lijuan; Journal of Chemical Research; vol. 39; 5; (2015); p. 296 – 299;,
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

22246-66-8, 5-Methoxyisoindolin-1-one is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,22246-66-8

To a suspension of (74) (7.07 g, 43.4 mmol) in CH2Cl2 (600 ml) was added BBr3(IM in CH2Cl2, 86.7 ml). The reaction mixture was stirred at room temperature for 4 hr. The solvent and boron residue was removed in vacuo and the remaining solid was dissolved in CH2Cl2, the solution was neutralized with 1 N NaOH (PH = 6.5). Desired compound was precipitated out and filtered. The organic solution was separated and washed with sat. NaCl, dried over Na2SO4 to give the title compound (combined weight 5.1 g, 78 %). MS (ES) m/z 150.1.

The synthetic route of 22246-66-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; WYETH; WO2006/138549; (2006); 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.1670-83-3,Indole-7-carboxylic acid,as a common compound, the synthetic route is as follows.

Example 18; Preparation of 1H-Indole-7-carboxylic acid (4-tert-butyl-benzyl)-[2-(3,4-dichloro-phenyl)-ethyl]-amide; To a solution of 48 mg (0.3 mmol) of 1H-indole-7-carboxylic acid and 96 mg of TBTU (0.3 mmol) in 4 ml DMF, were added 0.26 ml (1.5 mmol) of N,N-diisopropylethyl amine. After stirring for 5 min at rt, 95 mg (0.3 mmol) (4-tert-butyl-benzyl)-[2-(3,4-dichloro-phenyl)-ethyl]-amine in 1 ml DMF was added. After 1.5 h stirring at rt, the reaction mixture was diluted with 50 ml water and extracted with 2¡Á50 ml EtOAc. The combined organic phases were washed with water and brine, dried with magnesium sulfate, filtered and concentrated in vacuo. The yellow solid foam was purified by column chromatography (8 g silica gel; heptane/EtOAc 9:1) to give 137 mg (94%) of a white solid. MS (ISP) 479.5 (M+H)+., 1670-83-3

1670-83-3 Indole-7-carboxylic acid 74281, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Conte-Mayweg, Aurelia; Kuehne, Holger; Luebbers, Thomas; Maugeais, Cyrille; Mueller, Werner; Pflieger, Philippe; US2006/30613; (2006); 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