Day: August 27, 2020

4769-97-5, 4-Nitroindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-nitro-indole (1 equiv.) in dimethylformamide was added sodium hydride (1.50 equiv.) and benzenesulfonyl chloride (1.0 equiv.). The mixture was stirred at 0?30 C. for 2 h, and quenched with aqueous ammonium chloride at 0 C. The mixture was filtered, the solids were washed with water and petroleum ether, and the resulting solution was concentrated and dried in vacuo to give 4-nitro-1-(phenylsulfonyl)-1H-indole.

4769-97-5 4-Nitroindole 145766, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; PMV Pharmaceuticals, Inc.; Vu, Binh; Dominique, Romyr; Li, Hongju; (222 pag.)US2017/240525; (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.16732-70-0,Ethyl 5-bromo-1H-indole-2-carboxylate,as a common compound, the synthetic route is as follows.

Example 88 5-[l-(2-Oxo-pyrrolidin-l-yl)-ethyl]-lH-indole-2-carboxylic acid (3,5-difluoro-phenyl)- amide a) 5-ri-(2-Oxo-pyrrolidin-l-yl)-vinyll-lH-indole-2-carboxylic acid ethyl ester Palladium- (II) -acetat (17 mg) and tri-(o-tolyl)pho spine (68 mg) were dissolved in DMF (10 mL), then 5-bromo-lH-indole-2-carboxylic acid ethyl ester (400 mg), sodium hydrogen carbonate (501 mg), Nu,Nu-diisopropyl ethyl amine (1.02 mL) and l-vinyl-2-pyrrolidon (207 mg) were added. The reaction was stirred at 125C for 1.5 hours, followed by extraction with ethyl acetate and water. Column chromatography on silica gel using heptane / ethyl acetate (1: 1) yielded the title compound as the minor component of the reaction as a light grey solid (161 mg, 36 %). MS ISP (m/e): 299.2 (100) [(M+H)+].

As the paragraph descriping shows that 16732-70-0 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; BAUMANN, Karlheinz; FLOHR, Alexander; JOLIDON, Synese; KNUST, Henner; LUEBBERS, Thomas; NETTEKOVEN, Matthias; WO2014/60386; (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

4720-86-9, 4,5,6,7-Tetrahydro-1H-isoindole-1,3(2H)-dione is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a soln of 1 (1.40 g, 10.0 mmol) and Na2CO3 (1.06 g, 10.0 mmol) in H2O (10 mL), was added the dicarbonyl compound (10.0 mmol) and the mixture was refluxed for 15 min. The resulting clear solution was cooled and acidified with concd HCl (aq) soln (3 mL). The precipitate was filtered, washed with H2O (2 ¡Á 5 mL) and acetone (5 mL) and dried (100 C, 6 h).

The synthetic route of 4720-86-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Cal, Dariusz; Tetrahedron Letters; vol. 53; 29; (2012); p. 3774 – 3776;,
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.883535-89-5,2-(2-Methyl-1H-indol-1-yl)ethanamine,as a common compound, the synthetic route is as follows.

General procedure: A solution of 2-(2-methyl-1H-indol-1-yl)ethanamine (4a) (65 mg, 0.373 mmol) and 4-(piperidin-1-yl)benzoic acid (5) (76 mg, 1 eq.), and dimethylaminopyridine (catalytic, ?5 mg) in dichloromethane (6 mL) was added 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide.hydrochloride (EDCI) (92 mg, 1.3 eq.) at room temperature. The resulting reaction mixture was stirred for 6h. At the conclusion of the reaction (TLC), water (15 mL) was added to quench the reaction. The product was extracted with ethyl acetate (20mL¡Á3). Organics were washed with dilute HCl (10 mL), saturated NaHCO3 solution (10 mL), water (10 mL) and brine solution (10 mL) and dried over Na2SO4 and concentrated. The resulting crude product was subjected to silica gel chromatography eluting with 0-40% ethyl acetate in hexane to furnish 7k (TG7-152) (100mg, 74% yield). 1H NMR (CDCl3): delta 7.52 (d, J=5.6Hz, 1H), 7.49 (d, J=8.8Hz, 2H), 7.30 (d, J=8Hz, 1H), 7.07 (m, 2H), 6.80 (d, J=8.2Hz, 2H), 6.23 (s, 1H), 5.98 (t, J=5.4Hz, 1H), 4.33 (t, J=6Hz, 2H), 3.76 (q, J=6Hz, 2H), 3.25 (t, J=4.8Hz, 4H), 2.37 (s, 3H), 1.6 (m, 6H). LCMS (ESI): >97% purity at lambda 254, MS; m/z, 362 [M+H]+. Anal. Calcd. for C23H27N3O: C, 76.42; H, 7.53; N, 11.62; found; C, 76.48; H, 7.55; N, 11.59.

The synthetic route of 883535-89-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Ganesh, Thota; Jiang, Jianxiong; Dingledine, Ray; European Journal of Medicinal Chemistry; vol. 82; (2014); p. 521 – 535;,
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

16732-70-0, Ethyl 5-bromo-1H-indole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Ethyl 5-bromoindole carboxylate (1 ‘) (0.10 g, 0.373 mmol) was placed in a round bottom flask,10 mL of acetonitrile was added and 3,5-dimethylthiophenol (0.0516 g, 0.373 mmol, 50 muL) and 1-chloromethyl-4-fluoro-1,4-diazabicyclo [2.2. 2] octane bis (tetrafluoroborate) salt (0.10 g, 0.373 mmol).The reaction was continued for 6 hours.Acetonitrile was evaporated to dryness, 30 mL of water was added, the mixture was extracted with methylene chloride (3 ¡Á 10 mL)The organic phases were combined, washed with saturated brine and dried over anhydrous magnesium sulfate. Filtered and concentrated,Purification by column chromatography (ethyl acetate: petroleum ether = 1: 8).The resulting white solid was recrystallized from ethyl acetate / petroleum ether to give 2 ‘. Yield 50.5%.

16732-70-0 Ethyl 5-bromo-1H-indole-2-carboxylate 259091, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; Shandong University; Liu Xinyong; Li Xiao; Zhan Peng; (27 pag.)CN105968095; (2016); 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

6146-52-7, 5-Nitroindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0252] A solution of 5-nitroindole (10 g, 61.6 mmol) and acetyl chloride (5.8 g, 74 mmol) in methylene chloride at 0 C. is treated with tin tetrachloride (1 M in CH2Cl2, 68 mL), stirred under N2 for 6 h, treated with saturated NaHCO3 to pH 9 and filtered. The filtrate is concentrated in vacuo to give a residue. The residue is dissolved in DMF and filtered. This filtrate is concentrated in vacuo to give the title product, 12.6 g (99% yield), identified by NMR and mass spectral analyses.

The synthetic route of 6146-52-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Wyeth; US2003/232843; (2003); 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

2882-15-7, 5-Methoxy-2-methyl-3-indoleacetic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5-(((5-Methoxy-2-methyl-1H-indol-3-carbonyl)amino)methyl)-2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid; To a solution of 5-methoxy-2-methyl indole-3-acetic acid (0.26 g, 1.18 mmol), and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide, hydrochloride (0.27 g, 1.4 mmol) in acetonitrile (10 ml) was added triethylamine (0.46 ml, 3.2 mmol). The reaction mixture was allowed to stir for 10 min at room temperature before compound 2-amino-5-aminomethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid tert-butyl ester (0.307 g, 1.08 mmol) was added. The reaction mixture was allowed to stir for 18 hours and then concentrated in vacuo. Ethyl acetate and water were added and the layers separated. The organic layer was washed with hydrochloric acid (0.5M, (v/v)), saturated sodium bicarbonate (2¡Á25 ml) and brine (2¡Á25 ml). The organic layer was dried (MgSO4), filtered and concentrated in vacuo. The crude 2-amino-5-(((5-methoxy-2-methyl-1H-indol-3-carbonyl)amino-methyl)-4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid tert-butyl ester was used immediately in the next step.1H-NMR (CDCl3) delta 7.90 (bs, 1H), 7.19 (d, 1H, J=8.8 Hz), 6.87 (d, 1H, J=2.4 Hz), 6.79 (dd, 1H, J=8.8 Hz and J=2.4 Hz), 6.18 (m, 1H), 5.94 (s, 2H), 4.33 (m, 2H, J=25 Hz, J=14 Hz, J=2.8 Hz and J=1.6 Hz), 3.80 (s, 3H), 3.76 (ddd, 1H, J=14 Hz, J=8 Hz and J=2.8 Hz), 3.65 (s, 3H), 3.53 (m, 1H), 2.99 (ddd, 1H, J=13 Hz, J=5.6 Hz and J=4 Hz), 2.76 (dt, 1H, J =16.8 Hz, J=2.8 Hz), 2.42-2.40 (m, 1H), 2.38 (s, 3H), 1.51 (s, 9H).

As the paragraph descriping shows that 2882-15-7 is playing an increasingly important role.

Reference£º
Patent; Novo Nordisk A/S; US7019026; (2006); 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

883535-89-5, 2-(2-Methyl-1H-indol-1-yl)ethanamine is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A solution of 2-(2-methyl-1H-indol-1-yl)ethanamine (4a) (65 mg, 0.373 mmol) and 4-(piperidin-1-yl)benzoic acid (5) (76 mg, 1 eq.), and dimethylaminopyridine (catalytic, ?5 mg) in dichloromethane (6 mL) was added 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide.hydrochloride (EDCI) (92 mg, 1.3 eq.) at room temperature. The resulting reaction mixture was stirred for 6h. At the conclusion of the reaction (TLC), water (15 mL) was added to quench the reaction. The product was extracted with ethyl acetate (20mL¡Á3). Organics were washed with dilute HCl (10 mL), saturated NaHCO3 solution (10 mL), water (10 mL) and brine solution (10 mL) and dried over Na2SO4 and concentrated. The resulting crude product was subjected to silica gel chromatography eluting with 0-40% ethyl acetate in hexane to furnish 7k (TG7-152) (100mg, 74% yield). 1H NMR (CDCl3): delta 7.52 (d, J=5.6Hz, 1H), 7.49 (d, J=8.8Hz, 2H), 7.30 (d, J=8Hz, 1H), 7.07 (m, 2H), 6.80 (d, J=8.2Hz, 2H), 6.23 (s, 1H), 5.98 (t, J=5.4Hz, 1H), 4.33 (t, J=6Hz, 2H), 3.76 (q, J=6Hz, 2H), 3.25 (t, J=4.8Hz, 4H), 2.37 (s, 3H), 1.6 (m, 6H). LCMS (ESI): >97% purity at lambda 254, MS; m/z, 362 [M+H]+. Anal. Calcd. for C23H27N3O: C, 76.42; H, 7.53; N, 11.62; found; C, 76.48; H, 7.55; N, 11.59.

883535-89-5 2-(2-Methyl-1H-indol-1-yl)ethanamine 2049534, aindole-building-block compound, is more and more widely used in various.

Reference£º
Article; Ganesh, Thota; Jiang, Jianxiong; Dingledine, Ray; European Journal of Medicinal Chemistry; vol. 82; (2014); p. 521 – 535;,
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.1075-34-9,5-Bromo-2-methylindole,as a common compound, the synthetic route is as follows.

General procedure: 2-Methyl-1H-indole derivatives (0.5-6 mmol, 1 equiv) were stirred at 80 C in acetic acid (2 mL/1 mmol), 4-piperidone hydrochloride hydrate (1.5-18 mmol, 3 equiv) and 1 M phosphoric acid (1 mL/1 mmol) were added. After 1-2 h, the mixture was poured into ice/ammonia, and extracted with ethyl acetate (3 x 25 mL). The combined organic layers were washed with water and brine, dried, and evaporated in vacuo to give the title compounds. The crude products were purified by silica gel column chromatography (ethylacetate-methanol, gradient) and most of them were converted to the corresponding salts by dissolving the free base in methanol or ethanol and adding one equivalent of oxalic acid or ethanolic HCl solution. The solvent was removed and azeotroped with absolute ethanol in vacuo followed by recrystallization from appropriate solvents.

1075-34-9 5-Bromo-2-methylindole 5003968, aindole-building-block compound, is more and more widely used in various.

Reference£º
Article; Mattsson, Cecilia; Svensson, Peder; Boettcher, Henning; Sonesson, Clas; European Journal of Medicinal Chemistry; vol. 63; (2013); p. 578 – 588;,
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

10075-50-0, 5-Bromoindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Under a nitrogen stream , 5-bromo-1H-indole (25g, 0.13mol), Iodobenzene (31.22g, 0.15mol), Pd(OAc)2 (1.43g, 5.mol%), Triphenylphosphine (1.67g.5mol%), KOAc (37.55g, 0. Were mixed 38 mole ) and H2O (300ml), and stirred for 24 hours at 110 C. After completion of the reaction, and extracted with ethyl acetate , to remove water with MgSO4 , Karamukuro Chromatograph By (hexane :: EA = 10 1 (v / v 5-bromo-2-phenyl-1H-indole (16.66g, 48% yield) .

As the paragraph descriping shows that 10075-50-0 is playing an increasingly important role.

Reference£º
Patent; DOOSAN CORPORATION; KIM, HOE MOON; KIM, SUNG MOO; KIM, YOUNG BAE; KIM, TAE HYUNG; PARK, HO CHEOL; LEE, CHANG JUN; BACK, YOUNG MI; SHIN, JIN YONG; (222 pag.)JP2016/40292; (2016); 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