Day: September 23, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.198479-63-9,5-(Benzyloxy)-2-(4-(benzyloxy)phenyl)-3-methyl-1H-indole,as a common compound, the synthetic route is as follows.

In a 1000-L reactor, 90 kg of DMSO was added, and 30 kg of 5-(benzyloxy)-2-(4-(benzyloxy) was added at room temperature.Phenyl)-3-methyl-1H-indole was stirred until dissolution, 50 kg sodium hydroxide solids and 12 kg water were added,After activation for 1 h, a solution of compound 4 in DMSO (24 kg of compound 4 dissolved in 210 kg DMF) was added,After reacting for 1 hour at room temperature, the reaction is completed, 600 kg of purified water is added, and the crystals are stirred for 8 hours, filtered, and dried.This gave 42.8 kg of an off-white solid, yield: 91.8%, HPLC purity: 99.5%. .

198479-63-9, As the paragraph descriping shows that 198479-63-9 is playing an increasingly important role.

Reference£º
Patent; Yangzijiang Pharmaceutical Group Co., Ltd.; Wu Jianhua; Xu Jingren; Cai Wei; Zhu Xiaohe; Zhang Haibo; Lv Huimin; Hu Tao; Xiao Can; Gu Cheng; Xu Chenjun; (10 pag.)CN107793344; (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

36193-65-4, 1H-Indole-2-carbonitrile is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A Preparation of (26) where R10 is 2-Cyanoindole A mixture of 3.0 g (0.02 mol) of 2-cyanoindole, 4.2 g (0.02 mol) of tert-butyl-4-fluorobenzoate, and 5.5 g (0.04 mol) of potassium carbonate in 30 ml dimethyl sulfoxide was heated at 110 C. for 48 hours. The reaction was poured onto ice-water and extracted twice with ethyl acetate. The organic extracts were combined, washed with water and dried over magnesium sulfate. Evaporation yielded a dark oil which was flash chromatographed on silica gel, eluding with ethyl acetate-hexane 1:9 to give 3.6 g (0.011 mol) of 1-[4-(tertbutoxycarbonyl)phenyl]-2-cyanoindole as an oil.

36193-65-4, As the paragraph descriping shows that 36193-65-4 is playing an increasingly important role.

Reference£º
Patent; Syntex (U.S.A.) Inc.; US5380739; (1995); 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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4837-90-5,4-Methoxy-1H-indole,as a common compound, the synthetic route is as follows.

A. 1-Benzyl-4-methoxyindole NaH (7.7 g, 191.7 mmol) was added portionwise to a 0 C solution of 4-methoxyindole (21.7 g, 147 mmol) in 750 mL of anhydrous DMF. After 15 min, the slurry was treated with benzyl bromide (17.5 mL, 147 mmol). The reaction mixture was allowed to warm to ambient temperature and stir overnight. The reaction mixture was poured into 1 L of H2O. The layers were separated, and the aqueous phase was extracted with EtOAc (2 X 200 mL). The combined organic layers were washed with H2O (4 x 500 mL), dried over Na2SO4, filtered and concentrated in vacuo.The crude residue was purified by flash chromatography (SiO2; hexanes) to give 32.9 g (138.6 mmol; 94%) of the title compound as a white solid. Electrospray MS 238 (M+1);

4837-90-5, As the paragraph descriping shows that 4837-90-5 is playing an increasingly important role.

Reference£º
Patent; ELI LILLY AND COMPANY; EP950661; (1999); 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

882679-96-1,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.882679-96-1,Methyl 4-bromo-1H-indole-6-carboxylate,as a common compound, the synthetic route is as follows.

Step a. To a solution of methyl 4-bromo-lH-indole-6-carboxylate (CAS Number 882679-96-1) (1.0 g, 3.95 mmol) in TFA (5 ml) was added triethylsilane (1.9 ml, 11.86 mmol) at rt. The reaction mixture was stirred at 60C for 45 min. The resulting reaction mixture was cooled to rt, poured into saturated NaHC03 solution (50 ml) extracted with EtOAc (3 x 30 ml). The combined organic layer was dried over Na2S04, filtered and concentrated under reduced pressure. The resulting residue was purified by flash chromatography (10% EtOAc in hexane) yielding methyl 4-bromoindoline-6-carboxylate (0.75 g, 29.4 mmol). LCMS: Method C, 2.31 min, MS: ES+ 256.3, 258.3; NMR (400 MHz, DMSO-d6) delta ppm 7.20 (d, J= 1.2 Hz, 1H), 6.94 (d, J=1.6 Hz, 1H), 6.19 (s, 1H), 3.80 (s, 3H), 3.54 (t, J=8.8 Hz, 2H), 2.97 (t, J=8.8 Hz, 2H).

The synthetic route of 882679-96-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MISSION THERAPEUTICS LIMITED; KEMP, Mark; STOCKLEY, Martin; JONES, Alison; (138 pag.)WO2017/9650; (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.24621-73-6,4-Chloro-1H-indole-2-carboxylic acid,as a common compound, the synthetic route is as follows.,24621-73-6

Step 1. 4-Chloro-N-methoxy-N-methyl-1H-indole-2-carboxamide A mixture of 4-chloro-1H-indole-2-carboxylic acid (from Ryan Scientific, 1.0 g, 5.1 mmol), O-(benzotriazol-1-yl)-N,N,N’,N’-tetramethyluronium hexafluorophosphate (2.9 g, 7.7 mmol) and triethylamine (3.6 mL, 26 mmol) in N,N-dimethylformamide (15 mL) was stirred at room temperature for 10 minutes. N,O-Dimethylhydroxylamine hydrochloride (0.75 g, 7.7 mmol) was added and the resulting suspension was stirred at room temperature overnight. The mixture was quenched with water and then extracted with EtOAc. The combined organic layers were dried over MgSO4, concentrated and purified on silica gel (eluting with 0-35% EtOAc in hexane) to give the desired product (0.35 g, 29%). LCMS calculated for C11H12ClN2O2(M+H)+: m/z=239.1; Found: 239.1.

24621-73-6 4-Chloro-1H-indole-2-carboxylic acid 90561, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Li, Yun-Long; Combs, Andrew P.; US2011/312979; (2011); 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.348640-06-2,4-Bromo-7-azaindole,as a common compound, the synthetic route is as follows.

c.HNO3 (0.93 mL) was added drop wise to a solution of a H2SO4 (0.64 mL) at 0 C. 4-Bromo-1H-pyrrolo[2,3-b]pyridine (2 g, 10.15 mmol) in c.H2SO4 (9 mL) was added slowly, keeping the temperature at 0 C. After addition the reaction was stirred for a further hour at 0 C. before pouring carefully onto rapidly stirring ice/H2O (100 mL). The suspension was stirred for 30 mins and then the solids separated via filtration. The filter cake was washed with copious amounts of H2O before drying in vacuo at 40 C., to afford the desired compound, 1.9 g, 77.3%

348640-06-2, As the paragraph descriping shows that 348640-06-2 is playing an increasingly important role.

Reference£º
Patent; Vernalis (R&D) Limited; Stokes, Stephen; Graham, Christopher John; Ray, Stuart Christopher; Stefaniak, Emma Jane; US2015/11533; (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

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.

The reagents used for each of the amide bond formation was amino core (4 mumol), carboxylic acid (4 mumol, 1 eq.), DIEA (5 mumol, 1.2 eq.) and HBTU (4.5 mumol, 1.1eq.). A stock of the amino core for synthesis of 102 members requires an amount in excess of 150 fold. Both the starting amino core and the carboxylic acids were prepared as a stock solution of DMSO in a concentration of 0.6 mmol/1500 muL and 4 mumol/10 muL, respectively. HBTU and DIEA were dissolved in DMSO as a concentration of 4.5 mumol/10 muL (V/V) and 5 mumol/10 muL (V/V), respectively. Each of the acid portion was firstly mixed with the solution of HBTU in a plastic tube for 30 sec, followed by the addition of a mixture of the solution of amino core (4 mumol, 10 muL) and DIEA (10 muL) in a total volume of 40 muL. All vials were shaken for 1 min ultrasonically for the subsequent series dilution., 1477-49-2

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

Reference£º
Article; Su, Yuan-Hsiao; Chiang, Li-Wu; Jeng, Kee-Ching; Huang, Ho-Lien; Chen, Jenn-Tzong; Lin, Wuu-Jyh; Huang, Chia-Wen; Yu, Chung-Shan; Bioorganic and Medicinal Chemistry Letters; vol. 21; 5; (2011); p. 1320 – 1324;,
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

913836-24-5, tert-Butyl 4-nitro-1H-indole-1-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,913836-24-5

To a stirred solution of 1-Boc-4-nitroindole (6.14 g, 23.4 mmol) in EtOH (100 mL) was added 10% Pd/C (614 mg) under N2. The resulting mixture was shaken under hydrogen (H2, 50 psi) at room temperature for 8 h. The mixture was filtered through a pad of Celite, and washed with EtOH. The filtrate was concentrated under reduced pressure to give the product 1-Boc-4-aminoindole as off-white solid (5.23 g, 96% yield). MS (ESI) m/z 233.2

913836-24-5 tert-Butyl 4-nitro-1H-indole-1-carboxylate 25307166, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Wyeth; US2009/227575; (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.6960-46-9,Ethyl 7-nitro-1H-indole-2-carboxylate,as a common compound, the synthetic route is as follows.,6960-46-9

Preparation 29: Synthesis of 7-(tetrahydro-pyran-4-ylamino)-1H-indole-2-carboxylic acidEthyl 7-nitroindole-2-carboxylate (2.5 g, 10.7 mmol) was dissolved in methanol (50 ml). 10% Pd/C (200 mg) was added, and the mixture was stirred for 1 h under hydrogen gas. The mixture was filtered through celite, and the filtrate was distilled under reduced pressure. The distillate was dissolved 1,2-dichloroethane (50 ml), and tetrahydro-4H-pyran-4-one (1.3 ml, 12.8 mmol) and sodium triacetoxyborohydride (3.4 g, 16.1 mmol) were added. The mixture was stirred for 8 h at room temperature. After completion of the reaction, water was added. The mixture was extracted with ethyl acetate, dried over anhydrous magnesium sulfate and filtered. The filtrate was distilled under reduced pressure and concentrated. The residue was purified by column chromatography. Thus obtained compound was dissolved in methanol (50 ml) and tetrahydrofuran (50 ml), 1N-sodium hydroxide (43 ml, 42.8 mmol) was added, and the mixture was stirred for 8 h at room temperature. 1N-hydrochloric acid solution was added, and the mixture was extracted with ethyl acetate, dried over anhydrous magnesium sulfate and filtered. The filtrate was distilled under reduced pressure to give the title compound (2.1 g, Yield 76%).1H-NMR (400 MHz, DMSO-d6); delta 12.87 (br s, 1H), 11.46 (s, 1H), 6.97 (d. J=2.0 Hz, 1H), 6.86 (d, J=1.6 Hz, 1H), 6.85 (s, 1H), 6.37 (m, 1H), 5.73 (br s, 1H), 3.90 (m, 2H), 3.61 (m, 1H), 3.50 (m, 2H), 2.00 (m, 2H), 1.48 (m, 2H)Mass spectrum (ESI, m/z): Calculated: 260.12, Found: 260.30

The synthetic route of 6960-46-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Kim, Soon Ha; Kim, Hyoung Jin; Chung, Chul Woong; Park, Heui Sul; Kwak, Hyo Shin; Kim, Sung Ho; Park, Jin Gu; US2010/291533; (2010); 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

4769-96-4, 6-Nitro-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[000423j To a stirred solution of compound 1 (1 g, 1 eq) in DMF (10 mL), NaH (0.22 1 g,1.5 eq) was added at 0 C followed by the addition of methyl iodide (2.3 mL, 3 eq) at same temperature. The reaction mixture was stirred at same temperature for 30 mm. The progress of the reaction was monitored by TLC. After completion of the reaction, the reaction mixture was diluted with water and extracted with ethyl acetate (3 X 25 mL). Combined organic extracts were washed with brine, dried over anhydrous sodium sulfate and evaporated under reduced pressure. The crude product was purified by column chromatography on silica gel 100-200 mesh using 20% EtOAc-hexane to afford the title compound 2.

4769-96-4, As the paragraph descriping shows that 4769-96-4 is playing an increasingly important role.

Reference£º
Patent; BIOMARIN PHARMACEUTICAL INC.; BHAGWAT, Shripad; WANG, Bing; LUEDTKE, Gregory R.; SPYVEE, Mark; (490 pag.)WO2016/57834; (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