Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.16732-69-7,Ethyl 7-bromo-1H-indole-2-carboxylate,as a common compound, the synthetic route is as follows.

a (R)-7-Bromo-1-(2-tert-butoxycarbonylamino-1-methyl-ethyl)-1H-indole-2-carboxylic acid ethyl ester The title compound was produced in accordance with the general method of example 12b) from 7-bromo-1H-indole-2-carboxylic acid ethyl ester and (S)-5-methyl-2,2-dioxo-[1,2,3]oxathiazolidine-3-carboxylic acid tert-butyl ester. Yellow oil. ISP-MS: m/e=425.3 and 427.3 (M+H+).

16732-69-7, 16732-69-7 Ethyl 7-bromo-1H-indole-2-carboxylate 7017885, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; Bentley, Jonathan M.; Hebeisen, Paul; Muller, Marc; Richter, Hans; Roever, Stephan; US2002/35110; (2002); 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.89245-41-0,4-Bromoindole-3-acetic Acid,as a common compound, the synthetic route is as follows.

89245-41-0, Example 7 methyl (4-bromo-1H-indol-3-yl)acetic acid To methanol (10 mL), thionyl chloride (0.76 mL) was added dropwise at -15 to -10C, followed by stirring for 30 minutes. To the mixture, (4-bromo-1H-indol-3-yl)acetic acid (, 1.32 g) was added, followed by stirring at room temperature for 2 hours. To the reaction mixture, an aqueous saturated sodium hydrogen carbonate solution was added, followed by extraction with ethyl acetate. The organic layer was washed in turn with water and saturated saline, dried and then concentrated. The residue was washed with diisopropyl ether/n-hexane (1:2) to obtain the titled compound having the following physical properties (1.26 g). TLC: Rf 0.41 (n-hexane: ethyl acetate = 1:1); 1H-NMR(CDCl3): delta 3.74 (s, 3H), 4.06 (s, 2H), 6.98 (t, 1H), 7.10 (d, 1H), 7.23-7.27 (m, 2H), 8.25 (brs, 1H).

As the paragraph descriping shows that 89245-41-0 is playing an increasingly important role.

Reference：
Patent; ONO PHARMACEUTICAL CO., LTD.; EP1852420; (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.20289-27-4,7-(Benzyloxy)-1H-indole,as a common compound, the synthetic route is as follows.

Intermediate 32 Preparation of N-acetyltryotophan acetic anhydride (0.5 ML, 5.2 mmol) was added to a slurry of Intermediate 31 (0.575 g, 2.6 mmol) and DL-serine (0.270 g, 2.6 mmol) in anhydrous acetic acid (5 ML) at room temperature under a nitrogen blanket.The resulting orange solution was heated to reflux and stirred for 24 hours.The cooled mixture then was concentrated under reduced pressure to provide the intermediate N-acetyltryptophan as dark red oil, which was used immediately without purification

20289-27-4, 20289-27-4 7-(Benzyloxy)-1H-indole 260798, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; Orme, Mark W.; Sawyer, Jason Scott; Daugan, Alain Claude-Marie; US2003/225092; (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

59908-47-3, 5-Chloro-1-methyl-1H-indole-2-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Version B: 780 mg of 1 d and 1747 mg of HATU were first dissolved in 10 ml DMSO. Next, 314 mg of 2-methoxyethylamine and 1080 mg of N,N-diisopropylethylamine were added. The mixture was stirred for 1 hr at RT. The reaction mixture was poured into water and extracted three times with ethyl acetate. The combined organic phases were washed with saturated sodium chloride solution, dried over sodium sulphate, filtered and concentrated. The residue was purified chromatographically on the Biotage SP4. Gradient: ethyl acetate/methanol 0-10%. Yield: 740 mg of the title compound. Analogously to Example 1b, Version B, 43 mg of the title compound was obtained from 100 mg of 71a and 89 mg of 5-chloro-1-methyl-1H-indol-2-carboxylic acid in DMF. 1H-NMR (400 MHz, DMSO-d6): delta [ppm], 1.29 (2H), 1.38-1.72 (2H), 2.26-2.43 (1H), 2.54 (3H), 2.71-3.21 (2H), 3.73 (3H), 3.84-4.18 (3H), 4.38 (3H), 6.59 (1H), 7.15-7.28 (2H), 7.47 (1H), 7.55 (1H), 7.65 (1H), 8.57 (1H), 8.83 (1H)., 59908-47-3

59908-47-3 5-Chloro-1-methyl-1H-indole-2-carboxylic acid 931711, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; LlNDENTHAL, Bernhard; BRAeUER, Nico; SERNO, Peter; ROTGERI, Andrea; FUHRMANN, Ulrike; BUCHMANN, Bernd; MENGEL, Anne; ROeHN, Ulrike; TER LAAK, Antonius; (221 pag.)US2016/89364; (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

393553-57-6, 6-Bromo-4-methoxy-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Description 8. 6-Ethenyl-4-(methyloxy)-1 H-indole (D8) To a solution of 6-bromo-4-(methyloxy)-1 H-indole (900 mg, 3.98 mmol) in 1 ,2- dimethoxyethane (20 ml_) was added tributylvinyltin (1.74 ml_, 5.96 mmol). The reaction mixture was degassed with argon and then treated with dichlorobis(tri-o tolylphosphine)palladium (153 mg, 0.19 mmol). The mixture was heated at 9O0C for 65 hours. The mixture was filtered through a pad of celite, washed with ethyl acetate and then the filtrate concentrated in vacuo. The product was purified by silica gel chromatography eluting with 2-50% ethyl acetate in hexane to yield the title compound (D8), (781 mg). LC-MS: MH+ = 174 (CnH11NO = 173), 393553-57-6

The synthetic route of 393553-57-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; GLAXO GROUP LIMITED; WO2009/103710; (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

14618-45-2, 3-(Trifluoroacetyl)indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2,2,2-trifluoro-1-(1H-indol-3-yl)ethanone (0.20 g, 0.938 mmol) in THF (1 mL) inan ice-bath was added sodium borohydride (71.00 mg, 1.877 mmol) under N2. Then boron trifluoridediethyl ether (0.357 mL, 2.815 mmol) was added dropwise. The reaction was let stirred for 2 h whilewarmed to room temperature. The mixture was poured into a mixture of ice-water and 5% aqueousNaHCO3 and extracted with ethyl acetate. The combined organics were concentrated. The residue waspurified by silica gel column chromatography to give the title compound (90 mg). LCMS m/z = 200.4[M+H]+; 1H NMR (400 MHz, CD3OD) delta ppm 3.57 (q, 2H, J = 11.1 Hz), 7.04 (t, 1H, J = 7.4 Hz), 7.12 (t, 1H, J= 7.3 Hz), 7.20 (s, 1H), 7.37 (d, 1H, J = 8.0 Hz), 7.54 (d, 1H, J = 7.9 Hz).

14618-45-2, As the paragraph descriping shows that 14618-45-2 is playing an increasingly important role.

Reference：
Article; Dang, Huong; Feichtinger, Konrad; Frazer, John; Grottick, Andrew J.; Kasem, Michelle; Le, Minh; Lehman, Juerg; Morgan, Michael E.; Ren, Albert; Sage, Carleton R.; Schrader, Thomas O.; Semple, Graeme; Unett, David J.; Whelan, Kevin T.; Wong, Amy; Zhu, Xiuwen; Bioorganic and medicinal chemistry letters; (2020);,
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

900514-08-1,900514-08-1, 5-Chloro-3-iodo-7-azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1 Preparation of 5-Chloro-3-iodo-1-triisopropylsilanyl-1H-pyrrolo[2,3-b]pyridine (40)5-Chloro-3-iodo-1H-pyrrolo[2,3-b]pyridine (39, 31.2 g, 0.112 mmol) was dissolved in N-methylpyrolidinone (800 mL) and NaH (60% dispersion, 4.93 g, 0.123 mol) was added at room temperature. The resulting mixture was stirred for 30 minutes. To this mixture was then added triisopropylsilylchloride (24.0 mL, 0.112 mol) and the resulting mixture was stirred for 2 hours. The reaction was quenched with water and extracted with ethyl acetate three times, washed by brine, dried, filtered, and concentrated in vacuo. The residue was subjected to silica gel flash chromatography (eluted by heptane to 5% ethyl acetate/heptane) to afford the desired compound (43 g, 88%) as a pale-yellow solid

The synthetic route of 900514-08-1 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Spevak, Wayne; Cho, Hanna; Ibrahim, Prabha N.; Shi, Shenghua; Mamo, Shumeye; Gillette, Samuel J.; Zhu, Hongyao; US2008/167338; (2008); 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

525593-33-3,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.525593-33-3,3-Bromo-5-nitroindole,as a common compound, the synthetic route is as follows.

General procedure: A mixture of 5-nitro-1H-indole (200mg, 1.23mmol) or its derivatives and dry DMF (5mL) was cooled to 0C and NaH (60mg, 1.23mmol) was added. After the addition, the reaction mixture was stirred at r.t. for 0.5-1h, then compound 4 (282mg, 1.23mmol) was added, and the reaction mixture was allowed to stirred for an additional 2h. After a sequence of extraction, wash, and concentration, the crude product compound 5 (222mg, 0.72mmol, 58.30%) was obtained and could be used in next step without further purifications [12].

As the paragraph descriping shows that 525593-33-3 is playing an increasingly important role.

Reference：
Article; Wu, Zeng; Yan, Ming; Hu, Shi-He; Yu, Zhi-Cheng; Zhu, Yong; Cheng, Ya-Dong; Liu, Hai-Chun; Zhang, Yan-Min; Yao, Si-Hui; Tang, Wei-Fang; Lu, Tao; Chinese Chemical Letters; vol. 25; 2; (2014); p. 351 – 354;,
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

14618-45-2, 3-(Trifluoroacetyl)indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In 50ml absolute diethyl ether 5g 2,2,2-trifluoro-1-(1H-indol-3-yl)-ethanone are dissolved. 15.6ml of a methyl magnesium bromide solution (3 molar, in diethyl ether) is added slowly while the reaction temperature is kept at -10C. The mixture is allowed to warm up to 20C and is stirred for 2 hours. The reaction mixture is then treated with saturated ammonium chloride solution and the organic layer separated. The aqueous phase is extracted with diethyl ether and the combined organic phases dried over magnesium sulfate. The organic phase is evaporated in vacuo to give 1,1,1-trifluoro-2-(1H-indol-3-yl)-propan-2-ol, which is used without further purification.

14618-45-2, 14618-45-2 3-(Trifluoroacetyl)indole 589126, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; Novartis AG; EP1783114; (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.1082040-57-0,Methyl 6-chloro-1H-indole-4-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of methyl 6-chloro-1H-indole-4-carboxylate (1000 mg, 4.77 mmol) in tetrahydrofuran (20 mL) was added allyl alcohol (0.324 mL, 4.77 mmol), and the mixture was degassed for 5 minutes by bubbling nitrogen. Triethylborane (1.431 mL, 1.431 mmol) and tetrakis(triphenylphosphine)palladium(0) (276 mg, 0.239 mmol) were added and the mixture was heated to 75 C and stirred at 75 C for 18 hours. The mixture was concentrated and the residue was purified using column chromatography (silica gel, 0 to 70% EtOAc in hexanes) to afford methyl 3-allyl-6-chloro-lH-indole-4-carboxylate (714 mg, 60%) as a white solid. LC-MS(ES) m/z = 250 [M+H]+., 1082040-57-0

1082040-57-0 Methyl 6-chloro-1H-indole-4-carboxylate 53399422, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED; MILLER, William Henry; ROMERIL, Stuart Paul; VERMA, Sharad Kumar; TIAN, Xinrong; WO2015/132765; (2015); 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