Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.10075-50-0,5-Bromoindole,as a common compound, the synthetic route is as follows.

General procedure: A round-bottomed flask containing (28mL, 370mmol) freshly distilled dimethylformamide (DMF) was cooled to 0C for about 30min and freshly distilled phosphorus oxychloride (8.41mL, 90mmol) was subsequently added with stirring to the DMF over a period of 30min. A solution of indole 19 (85.47mmol) in DMF (10mL, 130mmol) was added to the yellow solution over a period of 1h. The solution was stirred at room temperature till it become a yellow paste. At the end of the reaction, 30g of crushed ice was added to the paste with stirring to make a clear cherry-red aqueous solution. Sodium hydroxide solution (1N, 100mL) was added dropwise with stirring to this cherry-red solution. The resulting suspension was heated rapidly to 90C and allowed to cool at room temperature, after which it was refrigerated for overnight. The product was filtered, washed with water (2¡Á100mL) and air-dried to afford pure indole-3-carboxaldehydes 20 in 80-90% yields. Indole-3-carboxaldehyde, pale yellow solid; mp 194-196C (Lit. [37]196-197C).

10075-50-0, The synthetic route of 10075-50-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Tantak, Mukund P.; Klingler, Linus; Arun; Kumar, Anil; Sadana, Rachna; Kumar, Dalip; European Journal of Medicinal Chemistry; vol. 136; (2017); p. 184 – 194;,
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

120-72-9, 1H-Indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation 6 Methyl indolyl-3-glyoxylate A solution of indole (2.0 g, 1.70 mmol) in Et2O (20 mL) was cooled to 0-5C under N2and oxalyl chloride (1.5 mL 1.70 mmol) was added dropwise at <5C. The resultant yellow slurry was stirred 30 min. in the ice bath and was then cooled to -65C and a 25% wt. solution of sodium methoxide (7.8 mL, 3.4 mmol) was slowly added at <-58C. The reaction was then allowed to warm to room temperature, water was added (10 mL), and the resultant mixture filtered. The solid was dried at room temperature to give 3.21 g (93%) of the titled compound. NMR. MS (FD) m/z= 203 (M+, 100%). Analytical calculated for C11H9NO3C, 65.02; H, 4.46; N, 6.89. Found C, 64.93; H, 4.25; N, 7.03. 120-72-9, 120-72-9 1H-Indole 798, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; ELI LILLY AND COMPANY; EP825190; (1998); 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.108438-43-3,Methyl 1-methyl-1H-indole-3-carboxylate,as a common compound, the synthetic route is as follows.

EXAMPLE 3 Preparation of 1-methyl-3-indoloylguanidine hydrochloride The reaction was carried out in a manner similar to Example 1 except for using 1.00 g (5.29 mmol) of methyl 1-methyl-3-indolecarboxylate, 5.05 g (52.9 mmol) of guanidine hydrochloride and 50 ml of a methanol solution of 2.85 g (52.9 mmol) of sodium methoxide. Thus 0.48 g (35.9%) of 1-methyl-3-indoloylguanidine hydrochloride was obtained. M.P.: 252-253 C. 1H NMR (DMSO-d6) delta: 3.91 (3H, s), 7.25-7.37 (2H, m), 7.58-7.61 (1H, m), 8.15 (1H, dd, J=1.3, 6.6 Hz), 8.3 (2H, br-s), 8.6 (2H, br-s), 8.78 (1H, s), 11.8 (1H, br-s)., 108438-43-3

The synthetic route of 108438-43-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sumitomo Pharmaceutical Co., Ltd.; US6169107; (2001); 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

6245-89-2,6245-89-2, (1H-Indol-3-yl)-1-propanamine is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 39 6-Fluoro-2-{[3-(1H-indol-3-yl)-propylamino]-methyl}-2,3,8,9-tetrahydro-7H-1,4-dioxino[2,3-e]indol-8-one (R)-2-(Toluene-4-sulfonyloxymethyl)-6-fluoro-2,3,8,9-tetrahydro-7H-1,4-dioxino[2,3-e]indol-8-one (1.0 g, 2.5 mmole) and 3-(3-aminopropyl)indole (1.74 g, 10 mmole) were combined in 30 ml of dry DMSO and heated at 80¡ã-90¡ã C. for 4 hours under an argon atmosphere. After cooling to room temperature, the mixture was diluted with 500 ml of 1:1 ethyl acetate/hexane and washed with 250 ml of saturated aqueous sodium bicarbonate and with two 250 ml portions of water, dried over sodium sulfate, filtered and concentrated in vacuum. The residue was column chromatographed on silica gel using 0.5percent methanol/CHCl3 as eluant to give 0.33 g of the free base of the title compound as a pale yellow oil. This was crystallized from ethanol with the addition of one equivalent of fumaric acid to give 0.29 g of the (S) enantiomer of the title compound as a yellow solid fumarate, m.p. 133¡ã C.

The synthetic route of 6245-89-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; American Home Products Corporation; US5756532; (1998); 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

53330-94-2, 1-(1H-Indol-5-yl)ethanone is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,53330-94-2

[001242j Step C: Following the procedure in Example 5, Step E, the methyl ketone from Step B, dimethyl carbonate (0.46 mL, 5.5 mmol) and sodium hydride (220 mg, 60percent dispersion in mineral oil, 5.5 mmol) in THF (6 mL) afforded methyl methyl 3-(1H-indol-5-yl)-3- oxopropanoate as an off white powder (120 mg, 27percent). MS m/z 216.1 [M-Hf.

53330-94-2 1-(1H-Indol-5-yl)ethanone 40732, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; PTC THERAPEUTICS, INC.; F. HOFFMANN-LA ROCHE AG; QI, Hongyan; CHOI, Soongyu; DAKKA, Amal; KARP, Gary, Mitchell; NARASIMHAN, Jana; NARYSHKIN, Nikolai; TURPOFF, Anthony, A.; WEETALL, Maria, L.; WELCH, Ellen; WOLL, Matthew, G.; YANG, Tianle; ZHANG, Nanjing; ZHANG, Xiaoyan; ZHAO, Xin; GREEN, Luke; PINARD, Emmanuel; RATNI, Hasane; WO2013/119916; (2013); 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

189882-33-5, 6-Cyano-7-azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step A: Cyclopropyl(1H-pyrrolo[2,3-b]pyridin-6-yl)methanone In a round-bottomed flask under an argon atmosphere, 3 g (21 mmol) of 1H-pyrrolo[2,3-b]pyridine-6-carbonitrile are dissolved in 35 ml of anhydrous tetrahydrofuran. 5.35 ml (42 mmol) of trimethylsilyl chloride and 126 ml (126 mmol) of phenylmagnesium bromide (1M in tetrahydrofuran) are then added. The reaction mixture is stirred for 1 night at ambient temperature. It is then hydrolyzed with 100 ml of 2M ammonium chloride solution. The pH is then acidified to 1 using 10% hydrochloric acid and the mixture is stirred for 2 hours at ambient temperature. The pH of that solution is then brought to 9 using concentrated ammonium hydroxide solution. The aqueous phase is extracted twice with 100 ml of dichloromethane. The organic phases are dried over magnesium sulphate, filtered and evaporated under reduced pressure. The crude product is purified by chromatography on silica gel (petroleum ether/ethyl acetate: 9/1 then 8/2) to yield the title product in the form of a beige solid. Melting point: 159 C. MS: m/z=187 [M+H]+.

189882-33-5, The synthetic route of 189882-33-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; LES LABORATOIRES SERVIER; US2009/274674; (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.10241-97-1,5-Methyl-1H-indole-2-carboxylic acid,as a common compound, the synthetic route is as follows.

In a 50 mL round bottom flask equipped with a magnetic stirrerSelectfluor? (708 mg, 2.0 mmol, 2.0 eq), lithium carbonate (296 mg, 4.0 mmol, 4.0 eq)Then, acetonitrile (3.3 mL) and water (1.7 mL) were added as a solvent and stirred well under an ice bath to maintain the reaction temperature of -20 to 0 ¡ã C,5-methylindole-2-carboxylic acid (175 mg, 1.0 mmol, 1.0 eq) was added slowly; The reaction flask was sealed in an ice bath for 15 hours;After completion of the reaction, the reaction mixture was extracted twice with 20 mL of ether, the organic phases were combined and washed with saturated brine,Dried over anhydrous sodium sulfate; after drying, the organic solvent was dried under reduced pressure in an ice bath to obtain a crude product. The crude product was purified by analytical analysisOf n-pentane as eluant to give the final product: 2-fluoro-5-methyl-1-indoline as a white solid in 52percent yield.

10241-97-1, As the paragraph descriping shows that 10241-97-1 is playing an increasingly important role.

Reference£º
Patent; Central South University; Tang, Zhenyu; Yuan, Xi; Yao, Jianfei; (24 pag.)CN106397377; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.608-07-1,2-(5-Methoxy-1H-indol-3-yl)ethanamine,as a common compound, the synthetic route is as follows.

General procedure: To a solution of 5-methoxytryptamine (1.0 g, 5.3 mmol), aldehyde (6.3 mmol) in CH2Cl2 (10 mL) was added trifluoroacetic acid (0.7 mL). The reaction mixture was stirred at room temperature until the disappearance of the reactants (monitored by TLC). Then, the reaction mixture was adjusted to pH 7-8 with saturated aqueous NaHCO3 solution and extracted with CH2Cl2 (3 x 10 mL). The combined organic layer was dried over anhydrous Na2SO4, filtered, and concentrated under reduced pressure. The residue was purified by flash column chromatography on silica gel (eluent: petroleum ether/ethyl acetate) to afford 1q-1w.

608-07-1, 608-07-1 2-(5-Methoxy-1H-indol-3-yl)ethanamine 1833, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Zhao, Ziquan; Sun, Yan; Wang, Lilin; Chen, Xuan; Sun, Yanpei; Lin, Long; Tang, Yulin; Li, Fei; Chen, Dongyin; Tetrahedron Letters; vol. 60; 11; (2019); p. 800 – 804;,
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,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.

General procedure: General procedure (9): Nitroindole derivative (1 equiv) was dissolved in ethanol (30 ml_ for 20.40 mmol of starting material) and 10% palladium on carbon (10 mmol%) was added. The reaction flask was shaken under hydrogen at 30 psi using the Parr Shaker Hydrogenation Apparatus for 2.5 h. The reaction was filtered over celite and washed with ethyl acetate. The filtrate was concentrated in vacuo and purified by silica gel flash column chromatography to afford the aminoindole product. Intermediate 16 1/-/-indol-5-amine Intermediate 16 (2.7 g, 20.4 mmol) was prepared as a black solid from 5-nitro-1 /-/-indole (6.3 g, 38.9 mmol, 1 equiv) according to general procedure (9) using 1 :1 hexane/ethyl acetate as the eluent for flash silica gel column chromatography. Yield: 53%. 1H NMR (400 MHz, CDCI3) delta: 7.96 (bs, 1 H), 7.22 – 7.17 (m, 1 H), 7.13 (t, J = 2.8 Hz, 1 H), 6.97 – 6.94 (m, 1 H), 6.67 (dd, J = 8.5, 2.2 Hz, 1 H), 6.39 – 6.37 (m, 1 H), 3.49 (s, 2H).

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

Reference£º
Patent; NATIONAL UNIVERSITY OF SINGAPORE; LEE, Sang Hyun; DYMOCK, Brian William; KITAGAWA, Mayumi; SEE, Cheng Shang; (178 pag.)WO2016/200339; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.399-72-4,5-Fluoro-2-methylindole,as a common compound, the synthetic route is as follows.

5-Fluoro-2-methylindole (0.45Kg, 3.017mol, l.Owt), powdered potassium carbonate (1.251Kg, 9.05mol, 2.78wt) and acetonitrile (9.0L, 20vol) were charged to a 2OL EPO flange flask at 15 to 250C. Ethyl bromoacetate (0.671L, 2.67mol, 1.49vol) was added and the resulting suspension heated to and maintained at reflux for 18h after which time in-process check analysis by 1H NMR1 indicated 87% conversion. A further charge of ethyl bromoacetate (0.333L, 1.32mol, 0.74vol) and powdered potassium carbonate (0.626Kg, 4.53mol, 1.39wt) was made and reflux conditions established for a further 6 hours. In-process check by 1H NMR1 analysis indicated 98.4% conversion. The flask contents were allowed to cool to 15 to 250C over 16 hours. The solids were removed by filtration and the filter-cake washed with acetonitrile (2x IL, 2x 2vol). The combined filtrates were concentrated to dryness under vacuum at up to 4O0C (water bath) to provide crude Stage 1 as a brown oil (1.286Kg). The crude product was purified by dry flash chromatography using a gradient elution from heptanes to heptanes:toluene to toluene to give ethyl-(5-fluoro- 2-methylindolyl-l-acetate) as an off-white solid (0.573Kg, 80.7% theoretical, corrected for residual toluene). Mixed fractions were re-chromatographed as appropriate., 399-72-4

399-72-4 5-Fluoro-2-methylindole 2778715, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; OXAGEN LIMITED; WO2006/92579; (2006); 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