Month: November 2020

52488-36-5, 4-Bromo-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,52488-36-5

To a solution of 4-bromo-1H-indole (LXX) (10 g, 50.8 mmol, 1 eq), DMAP (622 mg, 5.1 mmol, 0.1 eq) and TEA (10.6 ml, 76.1 mmol, 3 eq) in DCM (200 mL) was added Boc2O (14.4 mL, 61 mmol, 1.2 eq) at 0C. The reaction was warmed to room temperature and stirred for 2 h. Water (200 mL) was added and the mixture was extracted with DCM twice. The solvent was evaporated under vacuum to give tert-butyl 4-bromo-1H-indole-1-carboxylate (LXXI) as white solid (11.4 g, 38.5 mmol, 76% yield). 1H NMR (CDCI3, 400 MHz) delta ppm 1.68 (s, 9H), 6.64 (d, J=4Hz, 1H), 7.17 (t, J=8.4Hz, 1H), 7.39 (d, J=7.6Hz, 1H), 7.64 (d, J=3.2Hz, 1H), 8.11 (d, J=8.0Hz, 1H); ESIMS found for C13H14BrNO2 m/z 297.1 (M+H).

52488-36-5 4-Bromo-1H-indole 676494, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; SAMUMED, LLC.; KC, Sunil, Kumar; WALLACE, David, Mark; CAO, Jianguo; CHIRUTA, Chandramouli; HOOD, John; (279 pag.)WO2017/23973; (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

91348-45-7, Ethyl 3-bromo-1H-indole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

91348-45-7, EXAMPLE 5OB ethyl 3-ortho-tolyl-lH-indole-2-carboxylateA mixture of EXAMPLE 31B (1.08 g), ortho-tolylboronic acid (1.1 g), (1,1′- bis(diphenylphosphino)ferrocene)dichloropalladium(II) (140 mg) in dimethoxyethane:2N aqueous Na2CO3 (25 mL:5 mL) was stirred under nitrogen at 😯 C for 16 hours, diluted with ethyl acetate and was washed with water and brine. The organic phase was dried (MgSO4), filtered, and concentrated. The concentrate was purified by flash chromatography on silica gel with 0-10% ethyl acetate/hexanes.

The synthetic route of 91348-45-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ABBOTT LABORATORIES; WO2008/130970; (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

113162-36-0, Methyl 4-fluoro-1H-indole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To methyl 4-fluoro-1 h-indole-2-carboxylate (1.21 1 mmol, 234 mg) in N,N-dimethylformamide (10 ml) at 0 C was added sodium hydride (1.817 mmol, 72.7 mg). The reaction mixture was stirred for one hour at room temperature before iodomethane (1.817 mmol, 0.1 13 ml, 258 mg) was added. After stirring for three hours water was added and the product was extracted with dichloromethane and concentrated in vacuo to give methyl 4-fluoro-1 -methyl-1 H-indole-2-carboxylate (264 mg).

113162-36-0, As the paragraph descriping shows that 113162-36-0 is playing an increasingly important role.

Reference£º
Patent; N.V. ORGANON; MAN de,, Adrianus Petrus Antonius; REWINKEL,, Johannes Bernardus Maria; JANS,, Christiaan Gerardus Johannes Maria; RAAIJMAKERS,, Hans Cornelis Andreas; WIJKMANS,, Jacobus Cornelis Henricus Maria; WO2011/95556; (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

703-80-0, 3-Acetylindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

703-80-0, A solution of 0.80 g (5 mmol) of 3-acetylindole in 30 mL of dry THF was added and 0.4 g (2 eq) of NaH in an amount of 60% was added to the flask at 0 C. The mixture was stirred for 15 minutes and 1.3 mL (2 eq) CH3I, the reaction was gradually warmed to room temperature, the reaction 2 hours,TLC showed the disappearance of raw materials; 0 C slowly added ice water to quench the reaction, extracted 2-3 times with ethyl acetate, saturated sodium chloride solutionWashed once, dried over anhydrous sodium sulfate, and evaporated under reduced pressure to obtain 0.73g white solid1- (1-methyl-1H-indol-3-yl) ethanone,Yield: 92.0%.

As the paragraph descriping shows that 703-80-0 is playing an increasingly important role.

Reference£º
Patent; Hebei University of Science and Technology; Zhang Zhiwei; Li Hailing; Liu Shouxin; Dong Yu; Feng Juan; Li Junzhang; (20 pag.)CN106977515; (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

659737-57-2, 6-Hydroxyisoindolin-1-one is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

l,l’-(Azodicarbonyl)dipiperidine (252 mg, 1.0 mmol) was added to a solution of (+/-)-trans- fert-butyl 3-(hydroxymethyl)-4-(4-methoxyphenyl)pyrrolidine-l-carboxylate [(+/-)B6, 160 mg, 0.52 mmol], 6-hydroxyisoindolinone (82 mg, 0.55 mmol) and tributylphosphine (0.37 mL, 1.5 mmol) in anhydrous tetrahydrofuran (12 mL) at 0 C under nitrogen, after which the mixture was slowly warmed to room temperature, stirring for a total of 12 h. The mixture was treated with diethyl ether (60 mL) and the solids were removed by filtration under reduced pressure. The filtrate solvents were removed under reduced pressure and the residue was purified by flash column chromatography on silica gel, eluting with dichloromethane/methanol (9: 1), to afford (+/-)-trans-tert-bu y 4-(4-methoxyphenyl)-3-{[(3- oxoisoindolin-5-yl)oxy]methyl}pyrrolidine-l-carboxylate [(+/-)B8] as a white solid (110 mg, 48%): LCMS (M+H) 439., 659737-57-2

659737-57-2 6-Hydroxyisoindolin-1-one 11528364, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; TREVENA, INC.; CROMBIE SPEERSCHNEIDER, Aimee; YAMASHITA, Dennis SHINJI; PITIS, Philip Michael; HAWKINS, Michael John; LIU, Guodong; MISKOWSKI DAUBERT, Tamara Ann; YUAN, Catherine C.K.; BORBO KARGBO, Robert; HERR, Robert Jason; ROMERO, Donna; (125 pag.)WO2018/152293; (2018); 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.166104-20-7,1-Boc-5-Aminoindole,as a common compound, the synthetic route is as follows.

Example 1; (A) A solution of the N-Boc protected amine (1 mmol) in TFE (2,2,2-trifluoroethanol) or HFIP (hexafluoroisopropanol) (5 mL) was placed in a sealed microwave vial. The reaction mixture was heated (100¡ãC or 150¡ãC) in a Biotage – Initiator.(TM). Sixty microwave reactor with stirring until the disappearance of the starting material was observed. After cooling to room temperature, the mixture was evaporated to dryness under reduced pressure. The crude product was purified by flash-column chromatography. 1H NMR and 13C NMR were measured on Bruker Avance DPX-300 NMR or Bruker Avance-300 NMR spectrometers, operating at a proton (1H) frequency of 300.13 MHz and carbon (13C) frequency of 75.43 MHz.Example 2 Following the procedure set forth in Example 1(A) above, indole derivatives were deprotected using TFE or HFIP in a microwave reactor at 150¡ãC as set forth in Table 1 below.

166104-20-7, 166104-20-7 1-Boc-5-Aminoindole 11593831, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; F. Hoffmann-La Roche AG; EP2070899; (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.6146-52-7,5-Nitroindole,as a common compound, the synthetic route is as follows.,6146-52-7

General procedure: To a solution of indoles 1a-i (10mmol) in dry tetrahydrofuran (THF; 25mL), NaH (30mmol) was added. After the mixture was stirred 30min, CH3I (30mmol) in 5mL THF was added dropwise under 0C. The reaction mixture was stirred at room temperature for 12h in the dark. Then the reaction mixture was cooled to room temperature,diluted with 30mL saturated NH4Cl solution, and extracted with EtOAc (3¡Á30mL). The organic layer dried over anhydrous MgSO4 and concentrated in vacuo. The pure products 2a-i was obtained by column chromatography on silica gel (Petroleum ether/EtOAc=20:1) with yield of 90%-99%.

As the paragraph descriping shows that 6146-52-7 is playing an increasingly important role.

Reference£º
Article; Xia, Qinqin; Bao, Xiaodong; Sun, Chuchu; Wu, Di; Rong, Xiaona; Liu, Zhiguo; Gu, Yugui; Zhou, Jianmin; Liang, Guang; European Journal of Medicinal Chemistry; vol. 160; (2018); p. 120 – 132;,
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.20289-26-3,4-Benzyloxyindole,as a common compound, the synthetic route is as follows.

7.0 g 4-benzyloxy-lH- indole (31.35 mmol) was dissolved in 60 mL dry DMF and 1.317 g NaH (32.92 mmol, 60 % on mineral oil) was added at 0 C. The mixture was stirred for 1 hour, then 6.09 g benzenesulfonyl chloride (34.48 mmol) was added dropwise and the mixture was stirred at 0 C until no further conversion was observed. Then it was diluted with water and extracted with DCM. The combined organic phases were dried over Na2S04, filtered and the filtrate was concentrated under reduced pressure and purified via flash chromatography using heptane and EtOAc as eluents to obtain l-(benzenesulfonyl)- 4-benzyloxy- indole. 1H NMR (400 MHz, DMSO-d6) delta: 7.97 (d, 2H), 7.72 (d, 1H), 7.69 (t, 1H), 7.59 (t, 2H), 7.54 (d, 1H), 7.47 (d, 2H), 7.39 (t, 2H), 7.33 (d, 1H), 7.27 (t,lH), 6.89 (d, 1H), 6.85 (d, 1H), 5.20 (s, 2H) MS (EI, 70 eV) m/z (% relative intensity, [ion]): 77 (32), 91 (100), 141 (18), 222 (6), 272 (11), 363 (10, [M+]), 20289-26-3

As the paragraph descriping shows that 20289-26-3 is playing an increasingly important role.

Reference£º
Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; BALINT, Balazs; CSEKEI, Marton; SZABO, Zoltan; SZLAVIK, Zoltan; KOTSCHY, Andras; CHANRION, Maia; GENESTE, Olivier; CHEN, I-Jen; DAVIDSON, James Edward Paul; MURRAY, James Brooke; SIPOS, Szabolcs; ONDI, Levente; PROSZENYAK, Agnes; (164 pag.)WO2016/207217; (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

16136-52-0, 4-Cyanoindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 1H-indole-4-carbonitrile (6) (5g, 35.17mmol) in THF (100mL) was added NaH (1.3g, 52.75mmol) at 0C. The mixture was stirred for 5min and benzenesulfonyl chloride (6.5g, 42.21mmol) was then added. The reaction was allowed to room temperature and stirred for an additional 30min and then poured into a precooled saturated aqueous NH4Cl solution (300mL). The aqueous phase was separated and extracted with ethyl acetate (100mL¡Á3); the combined organic layers were washed with water (100mL) and brine (100mL), dried over Na2SO4, filtered and evaporated in vacuo. The residue was recrystallized (EtOAc) to give the 1-(phenylsulfonyl)-1H-indole-4-carbonitrile (7) (7.4g, yield 75%, purity 98%). MS (ESI) m/z 283.1 [M+H]+., 16136-52-0

The synthetic route of 16136-52-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Wang, Xueyuan; Bai, Enhe; Zhou, Hui; Sha, Sijia; Miao, Hang; Qin, Yanru; Liu, Zhaogang; Wang, Jia; Zhang, Haoyang; Lei, Meng; Liu, Jia; Hai, Ou; Zhu, Yongqiang; Bioorganic and Medicinal Chemistry; vol. 27; 3; (2019); p. 533 – 544;,
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.348-36-7,Ethyl 5-fluoro-1H-indole-2-carboxylate,as a common compound, the synthetic route is as follows.

To a solution of ethyl 5-fluoro-2-indole,Diphenylphosphine oxide as a raw material,The reaction steps are as follows:To the reaction flask was added 0.102 g (0.5 mmol) of ethyl 5-fluoro-2-indole ethyl ester,Diphenylphosphine oxide 0.152(0.75 mmol), 0.201 g (0.75 mmol) of manganese acetate and 30 ml of acetic acid at 50 ¡ã C for 1 hour. After the reaction,The crude product was separated by column chromatography (petroleum ether: ethyl acetate = 4: 1) to give the title product (yield 91percent

348-36-7, 348-36-7 Ethyl 5-fluoro-1H-indole-2-carboxylate 2727899, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Soochow University (Suzhou); Zou Jianping; Xue Jianfei; Zhou Shaofang; Zhang Peizhi; (12 pag.)CN105037422; (2017); B;,
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