Day: August 21, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1670-82-2,1H-Indole-6-carboxylic acid,as a common compound, the synthetic route is as follows.

A magnetically stirred solution of 1 H-indole-6-carboxylic acid (5.00 g, 31 .02 mmol) in DMF (40 mL) was treated with potassium carbonate (4.29 g, 31 .02 mmol) and dropwise with methyl iodide (1 .93 mL, 31 .02 mmol). After stirring at room temperature for 3 h, the resulting mixture was diluted with diethyl ether (150 mL) then washed with water (2 x 100 mL) before being dried over magnesium sulphate, filtered and concentrated under reduced pressure. The ensuing residue was subjected to flash chromatography [silica, 20:80 v/v diethyl ether/hexane] and concentration of the appropriate fractions (Rf = 0.42) afforded methyl 1 H-indole-6-carboxylate (4.29 g, 83percent) as a light yellow crystalline solid. H NMR (400 MHz, chloroform-d) delta 8.71 (brs, 1 H), 8.19 (s, 1 H), 7.84 (dd, J = 8.4 and 1 .3 Hz, 1 H), 7.67 (d, J = 8.4 Hz, 1 H), 7.37 (t, J = 2.8 Hz, 1 H), 6.60 (s, 1 H), 3.95 (s, 3H); 13C NMR (100 MHz, chloroform-d) delta 168.5, 135.3, 131 .7, 127.8, 123.6, 120.9, 120.4, 1 13.7, 103.0, 52.1 ; (+)-LRESIMS m/z (rel. int.) 198 (100) [M + Naf; vmax 3337, 1680, 1617, 1569, 1508, 1438, 1335, 1290, 1262, 1220, 1205, 1 128, 1 1 15, 1084, 982, 91 1 , 828, 775, 736, 659 cm”1.

1670-82-2 1H-Indole-6-carboxylic acid 595230, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; BETA THERAPEUTICS PTY LTD; NELMS, Keats; SCHWARTZ, Brett; JACKSON, Colin; BANWELL, Martin; HAMMOND, Edward; (100 pag.)WO2018/107200; (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.244-63-3,9H-Pyrido[3,4-b]indole,as a common compound, the synthetic route is as follows.

[EXAMPLE 7: Target Compound 12]; [Show Image] Under a nitrogen stream, 9H-pyrido[3,4-b]indole (2.8 g), Target Compound 3 (2.47 g), a copper powder (1.06 g), potassium carbonate (4.6 g), and tetraglyme (8 mL) were allowed to react at 180¡ãC for 8 hours with stirring. After the completion of the reaction, chloroform was added to the reaction mixture. The insoluble matter was filtered off. After the filtrate was concentrated, the resulting precipitate was subjected to suspension washing with methanol and purified by silica-gel column chromatography (an ethyl acetate/methylene chloride mixture –> an ethanol/methylene chloride mixture) to yield Target Compound 12 (1.27 g). DEI-MS: m/z = 617 (M – H)+ DCI-MS: m/z = 619 (M + H)+ This compound had a glass transition temperature of 135¡ãC, a melting point of 221¡ãC, and a vaporization temperature of 499¡ãC. This compound was dissolved in toluene in an amount of 3 percent by weight or more. The difference in energy between the excited triplet state and the ground state of this compound was 2.96 eV.

The synthetic route of 244-63-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Mitsubishi Chemical Corporation; EP1956008; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.700-06-1,Indole-3-Carbinol,as a common compound, the synthetic route is as follows.

In order to confirm the antioxidant activity of the compounds, a DPPH method was employed. DPPH (l,l-diphenyl-2-picrylhydrazyl) is a chromogenic radical and thus, can be used to directly confirm the radical scavenging activity of the samples. The samples were dissolved in 4 ml of distilled water or solvent (methanol) and then, mixed well with 1 ml of 100 muM DPPH. Subsequently, the samples were incubated at room temperature for 30 minutes. The absorbance of the remaining DPPH was measured at 517 nm. As a blank of the present experiment, distilled water or solvent was used, and as a control, an experimental group composed only of DPPH in distilled water or solvent without the sample was used. Further, vitamin C was used as a positive control. As a result, the antioxidant activity was expressed as percentages of the absorbance of each hydrolysate relative to the absorbance of control, as calculated by the following equation 1.[81][82] (Experimental Equation 1)[83]RSAW = Ab5 f hydfKylate chi l00 Abs of Control[84] (RSA: Radical Scavenging Activity)[85]

700-06-1 Indole-3-Carbinol 3712, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; BIOSPECTRUM, INC.; WO2008/72941; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.83150-76-9,Octreotide,as a common compound, the synthetic route is as follows.

Embodiment 1 : Synthesis of D-Phe-c[Cys-Phe-D-Trp-Lys(Boc)-Thr-Cys]-Thr(ol); Into a round bottom flask, 100mg of octreotide was put and dissolved by adding 5mL of N,N-dimethylformamide. After the octreotide completely dissolved, 20muL of (Boc)2O was added to the flask. The mixture reacted at room temperature for 24 hours and then the solvent was extracted by using a vacuum system to obtain a crude product, D-Phe-c[Cys-Phe-D-Trp-Lys(Boc)-Thr-Cys]-Thr(ol). Finally, the crude product was purified by a high performance liquid chromatography through a column of Hibar 250-10 Lichrosorb RP-18 (7mum) produced by Merck & Co., Inc., with 0.1% of trifluoroacetic acid/H2O as an eluent and 40 minutes (80% ~ 10%) as analytic time. The resultant retention time was 29.4 minutes. The solution from the major peak was collected and then subjected to freeze dry to obtain solid white powder (72mg, yield: 70%) which was analyzed mass spectrometry as [M+H]+=1119Da.

The synthetic route of 83150-76-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Institute of Nuclear Energy Research, Atomic Energy Council; EP1935433; (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

271-34-1, 5-Azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1 [0675] To a solution of lH-pyrrolo[3,2-c]pyridine (LXXIV) (1 g, 8.47 mmol, 1.0 eq) in THF (10 mL) was added NaH (60% in mineral oil) (0.24 g, 10.2 mmol, 1.2 eq) at 0C. The mixture was stirred at 0C for 0.5 h. PhS02Cl (LXXV) ( 1.80 g, 10.2 mmol, 1.2 eq) was then added to the solution at 0C. The reaction was warmed to room temperature and stirred for 1 h. Aqueous NaHCC^ (30 mL) was added and then extracted with EtOAc (x 3). The organic phase was combined and dried over Na2SC>4. Removal solvents under reduced pressure gave 1 – (phenylsulfonyl)-lH-pyrrolo[3,2-c]pyridine (LXXVI) as a yellow solid. (1.52 g, 5.88 mmol, 69.4% yield). NMR (CDC13, 400 MHz) delta ppm 6.75 (d, J=3.6Hz, 1H), 7.48 (t, J=8Hz, 2H), 7.55 – 7.61 (m, 2H), 7.89 – 7.93 (m, 3H), 8.49 (d, J=6Hz, 1H), 8.88 (s, 1H); ESIMS found for C13H10N2O2S mlz 259.1 (M+H).

271-34-1 5-Azaindole 9220, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; SAMUMED, LLC.; KC, Sunil Kumar; WALLACE, David Mark; CAO, Jianguo; CHIRUTA, Chandramouli; HOOD, John; (261 pag.)WO2017/23984; (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

271-34-1, 5-Azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of lH-pyrrolo[3,2-c]pyridine (LXXIV) (1 g, 8.47 mmol, 1.0 eq) in THF (10 mL) was added NaH (60% in mineral oil) (0.24 g, 10.2 mmol, 1.2 eq) at 0C. The mixture was stirred at 0C for 0.5 h. PhS02Cl (LXXV) (1.80 g, 10.2 mmol, 1.2 eq) was then added to the solution at 0C. The reaction was warmed to room temperature and stirred for 1 h. Aqueous NaHCC (30 mL) was added and then extracted with EtOAc (x 3). The organic phase was combined and dried over Na2SC>4. Removal solvents under reduced pressure gave 1 – (phenylsulfonyl)-lH-pyrrolo[3,2-c]pyridine (LXXVI) as a yellow solid. (1.52 g, 5.88 mmol, 69.4% yield). NMR (CDCI3, 400 MHz) delta ppm 6.75 (d, J=3.6Hz, 1H), 7.48 (t, J=8Hz, 2H), 7.55 – 7.61 (m, 2H), 7.89 – 7.93 (m, 3H), 8.49 (d, J=6Hz, 1H), 8.88 (s, 1H); ESIMS found for Ci3HioN202S mlz 259.1 (M+H).

As the paragraph descriping shows that 271-34-1 is playing an increasingly important role.

Reference£º
Patent; SAMUMED, LLC; KC, Sunil Kumar; WALLACE, David Mark; CAO, Jianguo; CHIRUTA, Chandramouli; HOOD, John; (251 pag.)WO2017/24003; (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.83-34-1,3-Methyl-1H-indole,as a common compound, the synthetic route is as follows.

a) 1,3-Dimethyl-1H-indole To a stirred solution of 3-methylindole (15.0 g, 114 mmole) in dry DMF (200 mL) was added NaH (60% dispersion in oil, 5.0 g, 125 mmole) in portions. Gas evolution was observed. The mixture was stirred for 30 min, then iodomethane (8 mL, 129 mmole) was added in one portion. The reaction became exothermic and was cooled in an ice bath. After 16 hr at RT, the reaction was concentrated under vacuum and the residue was taken up in ethyl acetate. The solution was washed with H2O then with brine, dried (MgSO4), and concentrated to dryness. Purification by short path distillation under vacuum (bp 88-92C, 0.5 mmHg) gave the title compound (16.10 g, 97%) as a pale yellow oil: 1H NMR (400 MHz, CDCl3) delta 7.47 (d, J = 7.9 Hz, 1 H), 7.35 (d, J = 8.2 Hz, 1 H), 7.13 (t, 1 H), 7.06 (s, 1 H), 7.00 (t, 1 H), 3.71 (s, 3 H), 2.24 (s, 3 H).

83-34-1 3-Methyl-1H-indole 6736, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; Affinium Pharmaceuticals, Inc.; EP1226138; (2004); 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

61-54-1, 2-(1H-Indol-3-yl)ethanamine is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a refluxing suspension of tryptamine (CAS number 61 -54-1 , available from Combi blocks) (1 .00 g, 6.240 mmol) in 5% trifluoroacetic acid in acetonitrile (100 ml) was added solution of aqueous formaldehyde (37% w/v, 0.50 ml, 6.240 mmol) in acetonitrile (25 ml) drop wise over a period of 30 min and the resulting reaction mixture was allowed to reflux for 24 h. The resulting reaction mixture was cooled to ambient temperature, concentrated under reduced pressure and poured into saturated solution of NaHCC>3 (50 ml) and extracted with ethyl acetate (4 x 25 ml). The combined organic phase was dried over Na2S04, filtered and concentrated under reduced pressure yielding 2,3,4,9-tetrahydro-1H -3-carboline (1.00 g, 5.81 1 mmol) which was used further synthesis without further purification. LCMS: Method B: 3.681 min. MS: ES 173.5 (M+1 ).

As the paragraph descriping shows that 61-54-1 is playing an increasingly important role.

Reference£º
Patent; ARGONAUT THERAPEUTICS LIMITED; MORLEY, Andrew; MILLER, Rebecca; LA THANGUE, Nicholas; (126 pag.)WO2018/167276; (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

61-54-1, 2-(1H-Indol-3-yl)ethanamine is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Firstly, glyoxylic acid monohydrate (12.66 g, 137.6 mmol) was mixed with and dissolved in deionized water (30.00 mL). Tryptamine (20.0 g, 124.5 mmol) was also mixed and stirred with deionized water (380.00 mL), followed by adding several drops of hydrochloric acid. The two water solutions prepared as above were mixed and stirred for 15 minutes at room temperature, and a large amount of white precipitation was formed. In addition, a potassium hydroxide solution was prepared by dissolving potassium hydroxide (KOH, 6.8 g) in deionized water (34.00 mL). The potassium hydroxide solution was slowly added by drops into the mixed solution containing glyoxylic acid monohydrate and tryptamine, followed by adjusting the pH value of the solution to around 4 by hydrochloric acid. The mixture was stirred for one hour at room temperature and was allowed to stand in a freezer for 12 hours. After taken out from the freezer, the mixture was filtered by suction to collect solid, followed by added with deionized water (320.00 mL) and hydrochloric acid (60.00 mL). After refluxed for 30 minutes, the mixture was added with hydrochloric acid (60.00 mL) and refluxed again for 15 minutes, followed by cooling to room temperature. The mixture was allowed to stand in the freezer for two days for precipitation. The solid was collected and then added with deionized water. The mixture was heated to 165 C. to dissolve the solid and a dark green solution was formed. The pH value of the solution was adjusted to 12 by adding potassium hydroxide and a large amount of ligh green precipitation was formed. The solid was filtered by suction and the compound 3 (18.19 g) was obtained. The yield is 80%. Spectral data as follow: 1H NMR (400 MHz, d6-DMSO) : delta 6 10.67 (s, 1H), 7.34 (d, J=7.6 Hz, 1H), 7.26 (d, J=8.0 Hz, 1H), 6.99 (m, 1H), 6.94-6.93 (m, 1H), 3.86 (s, 2H), 3.08 (br s, 2H), 2.98 (t, J=5.2 Hz, 2H), 2.59 (m, 2H) ; 13C NMR (100 MHz, d6-DMSO) : delta 134.99, 133.68, 126.76, 119.67, 117.60, 116.64, 110.27, 106.42, 42.87, 42.14, 21.67. The reaction was shown as the following Equation (5).

61-54-1 2-(1H-Indol-3-yl)ethanamine 1150, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; Yuan Ze University; TING, Pei-Ling; LEUNG, Man-Kit; CHIU, Tien-Lung; LEE, Jiun-Haw; YUN, Lik-Ka; (14 pag.)US2017/162794; (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

95-20-5, 2-Methylindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1. 5-Bromo-2-methyl-7H-indoleTo a solution of 2-methyl-iH-indole (5.0 g, 38.12 mmol) in sulfuric acid (80 mL) was added Ag2S04 (12.5 g, 40.06 mmol) with ice cooling, and the solution was stirred for 30 min. Then Br2 (6.4 g, 40.05 mmol) was added to the solution dropwise over 30 min. After the solution was stirred for 4 h at room temperature, the reaction was then quenched by the addition of water/ice (300 mL). The reaction mixture was extracted with dichloromethane (3 x 200 mL) and the organic layers combined, dried over anhydrous sodium sulfate and concentrated in vacuo to afford 5-bromo-2-methyl-7H-indole as a light brown solid (6 g, 75%).LC/MS (ES, m/z): [M+H]+ 211.0’H-NMR (300 MHz, CDC13): delta 11.23 (s, 1Eta), 7.56 (s, 1Eta), 7.21 (d, / = 8.7 Hz, 1H), 7.07 – 7.09 (m, 1H), 6.11 (s, 1H), 2.38 (s, 3H)

The synthetic route of 95-20-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOENERGENIX; MCCALL, John M.; ROMERO, Donna L.; KELLY, Robert C.; WO2012/119046; (2012); 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