Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.942-26-7,5-Chlorotryptamine hydrochloride,as a common compound, the synthetic route is as follows.,942-26-7

EXAMPLE 113 – PREPARATION of N-(2-(5-Chloro-1 H-indol-3-yl)ethyl)-4-(3- fluorophenoxy)benzamide. A solution of 4-(3-fluorophenoxy)benzoic acid(0.180 g, 0.775 mmol), 2-(5-chloro-1 H- indol-3-yl)ethanamine hydrochloride (0.180 g; 0.775 mmol), HATU (0.324 g; 0.852 mmol) and Nu,Nu-diisopropylethylamine (0.334mL; 1.94 mmol) in DMF (5 mL), was stirred at room temperature overnight. The reaction mixture was partitioned between ethyl acetate and sodium hydrogen sulfate, the organic layer was washed with sodium carbonate, brine, dried and concentrated under reduced pressure. The crude mixture was purified by flash chromatography on silica (eluent 2 to 20 % ethyl acetate in dichloromethane and 20 to 100% ethyl acetate in heptane ) to yield 0.065 g (20%) of the title compound as a white solid.ESI/APCI(+):409 (M+H); ESI/APCI(-): 407 (M-H).

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

Reference£º
Patent; KATHOLIEKE UNIVERSITEIT LEUVEN, K.U. LEUVEN R&D; REMYND; GRIFFIOEN, Gerard; VAN DOOREN, Tom; ROJAS DE LA PARRA, Veronica; ALLASIA, Sara; MARCHAND, Arnaud; KILONDA, Amuri; CHALTIN, Patrick; WO2012/80221; (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

168824-94-0, tert-Butyl 3,4-dihydro-1H-pyrido[3,4-b]indole-2(9H)-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Excess 1,3-dibromopropane and methyl 2-(4-hydroxyphenyl)acetate are reacted in ethanol to give compound 25.Compound 6 was dissolved in DMF,After pulling with NaH hydrogen,Add compound 25,The compound 26 is obtained by reacting at normal temperature.Compound 26 was dissolved in DCM.Join TFA,Reaction under ice bath conditions gave compound 27.

168824-94-0, The synthetic route of 168824-94-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Second Military Medical University; Liu Na; Sheng Chunquan; Jiang Yanjuan; Tu Jie; Li Zhuang; Dong Guoqiang; Wu Shanchao; (31 pag.)CN108623585; (2018); 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

868656-97-7, Methyl 6-bromo-1H-indole-3-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

868656-97-7, Intermediate Preparation 41; 6-Bromo-l -methyl- IH- indole-3-carboxylic acid methyl ester; To a mixture of 6-bromo- leta-indole-3-carboxylic acid methyl ester (100 mg, 0.394 mmol), potassium carbonate (163 mg, 1.18 mmol) in DMF is added iodomethane (30 muL, 0.47 mmol). The reaction mixture is stirred for 1.5 h. Additional iodomethane (10 muL) is added and the reaction is stirred for 30 minutes. The reaction mixture is diluted with dichloromethane and filtered. The filtrate is concentrated under high vacuum, diluted with ethyl acetate, and concentrated to give the title compound (105 mg, 99%). ES/MS m/e 270.0 (M + 2).

868656-97-7 Methyl 6-bromo-1H-indole-3-carboxylate 11499811, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; ELI LILLY AND COMPANY; WO2009/12125; (2009); 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

230291-43-7, Methyl 4-chloro-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 solution of methyl 4-chloro-li -indole-2-carboxylate (5.30 g, 25.2 mmol) and potassium carbonate (10.4 g, 75.8 mmol) inN,N-dimethylformamide (70.0 mL) was added methyl iodide (10.7 g, 75.8 mmol) and the reaction mixture was stirred at 60 C for 4 hrs. On completion, the reaction mixture was concentrated in vacuo to give a crude product, which was purified by silica gel chromatography (petroleum ether : ethyl acetate = 5: 1) to give the title compound. NMR (400MHz, DMSO-d6) delta = 7.63 (d, J= 8.4 Hz, 1H), 7.36 (t, J= 8.0 Hz, 1H), 7.28 – 7.17 (m, 2H), 4.06 (s, 3H), 3.88 (s, 3H).

230291-43-7, The synthetic route of 230291-43-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; RAZE THERAPEUTICS, INC.; MAINOLFI, Nello; (358 pag.)WO2017/156165; (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.98600-34-1,4-Bromoindole-3-carboxyaldehyde,as a common compound, the synthetic route is as follows.

-Acetyl-4-bromo-l,2-dihydro-indol-3-one: 4-Bromo-lH-indole-3-carbaldehyde (4.0 g, 17.8 mmol) was stirred in acetic anhydride (20 mL) at reflux for 4h. The reaction was cooled and concentrated in vacuo. Cold MeOH was added to precipitate a white solid, whi, 98600-34-1

98600-34-1 4-Bromoindole-3-carboxyaldehyde 2763178, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; WO2009/129401; (2009); 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.98600-34-1,4-Bromoindole-3-carboxyaldehyde,as a common compound, the synthetic route is as follows.

Example 43 N4-(5-Cyclopropyl- 1 H-pyrazol-3 -yl)-N2-((3 -methyl- 1 H-indol-4-yl)methyl)pyrimidine-2,4-diamine (1-92) step 1 : To a refluxing solution of 4-bromo-lH-indole-3-carbaldehyde (644 mg, 2.87 mmol) in dry THF (20 mL) was added LiAlH4 (218 mg, 5.75 mmol) in several small portions. Heating at reflux was continued for 1 h, the reaction cooled to RT and quenched with water (220 mu?^), 15 % aq. NaOH (w/w, 220 mu? ), and water (650 mu?^). The resulting precipitate was filtered and the filtrate was concentrated under reduced pressure to dryness. To the residue was added aq. NaOH (10 mL) and the solution twice extracted with DCM (2 x 10 mL). The combined extracts were dried (MgSO i), filtered and concentrated in vacuo to afford 454 mg (75%) of 4-bromo-3 -methyl- lH-indole (230) as light brown oil: MS (ESI) m/z = 210.1 [M+l] +, 98600-34-1

As the paragraph descriping shows that 98600-34-1 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; ALIAGAS-MARTIN, Ignacio; CRAWFORD, James; LEE, Wendy; MATHIEU, Simon; RUDOLPH, Joachim; WO2013/26914; (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

81224-16-0, 7-Bromo-4-methoxy-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

81224-16-0, To a flame-dried flask containing 10a5 (50.0 mg, 0.233 mmol) in anhyd. THF (600 muL), added oxalyl chloride (97 muL, 1.11 mmol, 5 equiv) and let stir under an atmosphere of N2 until TLC (5:1 hexanes/EtOAc) indicated consumption of starting material (5-12 hr, depending on scale). All volatiles were removed by rotoevaporation and resulting green residue was immediately suspended in anhyd. THF (1 mL), followed by the addition of N-Boc piperazine6 (52 mg, 0.28 mmol, 1.2 equiv) and DIPEA (78 muL, 2 equiv). Resulting mixture was stirred under an atmosphere of N2 at RT for 12 hr. and then at reflux for 30 min (if needed) when TLC (5:1 hexanes/EtOAc) indicated reaction completion. Reaction was allowed to cool to RT, poured into H2O (10 mL) and extracted with EtOAc (3¡Á10 mL). The combined organic layers were dried over anhyd. MgSO4, filtered, and all solvents were evaporated. Crude 18 was purified by flash chromatography (CombiFlash Automated Chromatographer, 12 g column, dryloaded with 4 g pre-packed dry loading column. Run using 100% Hexanes to 50% EtOAc:Hexanes gradient over 30 column volumes, followed by EtOAc flush) to yield 18 as a light brown powder (78 mg, 75%). 1H NMR (400 MHz, CDCl3) delta 9.44 (s, 1H), 7.94 (d, J=3.1, 1H), 7.28 (d, J=8.5, 1H), 6.56 (d, J=8.5, 1H), 3.90 (s, 3H), 3.71 (m, 2H), 3.60-3.51 (m, 2H), 3.46 (m, 4H), 1.47 (s, 9H). (ES+) m/z (M+H)+ 466; (M+Na)+ 488; Rt=1.34. 5. US PATENT: US200300692456. Faust, A.; Waschkau, B.; Waldeck, J.; Holtke, C.; Breyholtz, H.; Wagner, S.; Kopka, K.; Heindel, W.; Schafer, M.; Bremer, C. Bioconjug. Chem. 2008, 19, 1001-1008.

As the paragraph descriping shows that 81224-16-0 is playing an increasingly important role.

Reference£º
Patent; Yale University; US2012/269766; (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

111258-23-2, Methyl 4-methoxy-1H-indole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,111258-23-2

Example 27A Methyl 1-cyanomethyl-4-methoxy-1H-indole-2-carboxylate Starting with 5.0 g (24.4 mmol) of methyl 4-methoxyindole-2-carboxylate, the general procedure [K] gives 5.6 g (92% of theory) of product. HPLC (method 1): Rt=4.34 min MS (ESIpos): m/z=245 (M+H)+

111258-23-2 Methyl 4-methoxy-1H-indole-2-carboxylate 688172, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Bayer HealthCare AG; US2007/185121; (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.1211594-25-0,4-Bromo-1H-indole-7-carboxylic acid,as a common compound, the synthetic route is as follows.

A solution of 4-bromo-1H-indole-7-carboxylic acid (5.5 g, 22.91 mmol) EDC (6.59 g, 34.4 mmol) and HOBt (5.26 g, 34.4 mmol) in THF (150 mL) and DCM (180 mL) was stirred at rt for 1 h. The mixture was then bubbled with NH3 gas for about 15 mm and the resulting mixture was stirred at rt overnight. The mixture was diluted by addition of water and extracted with DCM. The organic phase was washed with brine, dried and concentrated to give a residue, which was suspended in ether and filtered to provide 4-bromo-]H-indole-7-carboxamide (5.3 g, 97%): ?H NMR (DMSO-d6) 3 11.40 (br, 1H), 8.08 (br, 1H), 7.29-7.57 (d, J = 7.6 Hz, 1H), 7.43-7.42 (m, 2H), 7.28-7.26 (d, J = 7.6 Hz, 1H), 6.43-6.42 (m, 1H)., 1211594-25-0

1211594-25-0 4-Bromo-1H-indole-7-carboxylic acid 59267539, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; ABBVIE INC.; BONAFOUX, Dominique; DAVIS, Heather, M.; FRANK, Kristine, E.; FRIEDMAN, Michael, M.; HEROLD, J., Martin; HOEMANN, Michael, Z.; HUNTLEY, Raymond; OSUMA, Augustine; SHEPPARD, George; SOMAL, Gagandeep, K.; VAN CAMP, Jennifer; VAN EPPS, Stacy, A.; VASUDEVAN, Anil; WALLACE, Grier, A.; WANG, Lu; WANG, Zhi; WILSON, Noel, S.; XU, Xiangdong; WO2014/210255; (2014); 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

318-54-7, 2,2,2-Trifluoro-1-(1-methyl-1H-indol-3-yl)ethanol is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 15: 2,2,2-Trifluoro-l-(l-methyl-lH-indol-3-yl)-l-(l-pyridin-3-yl-lH-indazol-5- yl)ethanol; To a chilled (-780C) solution of 1.5 g (7.61 mmol) of 5-bromoindazole in 15 mL ether was added 9.2 mL (23.0 mmol) of a 2.5 M solution of n-butyllithium in hexanes. After 5 minutes, the cold bath was removed and the mixture stirred 6 hours at room temperature. The mixture was cooled to -78C and 3.5 g (15.4 mmol) of 2,2,2-trifluoro-l-(l-methyl-lH-indol-3- yl)ethanone in 4 mL of a 1: 1 mixture of ether-TetaF was added. The mixture was stirred overnight while warming to room temperature and was then quenched with aqueous ammonium chloride and extracted with ether. The organic layer was washed with water, brine, and dried over magnesium sulfate. Removal of the volatiles in vacuo provided a residue which was purified by CombiFlash chromatography using 0-90% EtOAc-hexanes (product eluted at 35% EtOAc) to afford 700 mg (26%) of 2,2,2-trifluoro-l-(lH-indazol-5-yl)-l-(l-methyl-lH-indol-3- yl)ethanol as a pale yellow foam.

318-54-7, As the paragraph descriping shows that 318-54-7 is playing an increasingly important role.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG; WO2008/70507; (2008); 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