Day: October 27, 2020

608-07-1, 2-(5-Methoxy-1H-indol-3-yl)ethanamine is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: In an 5 ml RB flask with refluxing condensor were added a mixtureof 4-nitrobenzaldehyde (2a, 33 mg, 0.22 mmol, 1.1 equiv.,), tryptamine(1a, 32 mg, 0.20 mmol, 1 equiv.,) in NMP (1 ml) under oxygen atmosphereand the resulting mixture was stirred at 140 C for 24 h. After thereaction was complete, the reaction mixture was concentrated underreduced pressure using rotary evaporator. The crude product thus obtainedwas purified by flash column chromatography on silica gel usingmixture of hexane-ethyl acetate (70:30) as eluent to obtain the product6a as Yellow solid; 91% yield (53.3 mg, 0.182 mmol); mp:244-246 C(Lit.20: 243-246 C);.

608-07-1, As the paragraph descriping shows that 608-07-1 is playing an increasingly important role.

Reference£º
Article; Ramu; Srinath; kumar, A. Aswin; Baskar; Ilango; Balasubramanian; Molecular catalysis; vol. 468; (2019); p. 86 – 93;,
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

80360-20-9, 1-(Phenylsulfonyl)-1H-indole-3-carbaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Thiosemicarbazide (1 mmol) and potassium hydroxide(1 mmol) were dissolved in 10 mL ethanol and stirred for 30 min.The resulting solution was added to a solution of compound 5a(1 mmol) in 10 mL ethanol. The mixturewas stirred at 110 C for 3 h.The reaction was cooled, which resulted in a white precipitate thatwas then recrystallized in alcohol to obtain compound 8a. Thecompounds 8b-8l were obtained using the same method as that for8a., 80360-20-9

As the paragraph descriping shows that 80360-20-9 is playing an increasingly important role.

Reference£º
Article; Song, Mingxia; Wang, Shiben; Wang, Zengtao; Fu, Zhiyang; Zhou, Shengchao; Cheng, Huabin; Liang, Zhuo; Deng, Xianqing; European Journal of Medicinal Chemistry; vol. 166; (2019); p. 108 – 118;,
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.26340-49-8,2-Iodo-1H-indole,as a common compound, the synthetic route is as follows.

To a solution of 6 (6.97 g, 28.68 mmol) in CH2Cl2 (96 mL) at 0 C was added methyl vinyl ketone(4.02 g, 57.35 mmol) and InCl3 (0.32 g, 1.45 mmol). The mixture was stirred at 0 C for 1 h and warmedto RT. After 3 h, the reaction mixture was quenched with sat. aq. NaHCO3 (80 mL) and extracted withCH2Cl2 (2 x 80 mL). The organic layers were combined, washed with brine (80 mL), dried over MgSO4,and concentrated in vacuo. The residue was purified by recrystallization from hexane/CH2Cl2 (5:1, 30mL) to afford 7 (7.38 g, 82% yield) as a light yellow crystal. The filtrate was concentrated in vacuo andthe residue was purified by flash chromatography (silica gel, hexane/AcOEt = 6:1) to afford 7 (0.75 g,8% yield) as a light yellow crystal. Keto indole 7 was prepared in total 90 % yield.

26340-49-8, The synthetic route of 26340-49-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Miyamoto, Hiroshi; Hirano, Tomohiro; Okawa, Yoichiro; Nakazaki, Atsuo; Kobayashi, Susumu; Tetrahedron; vol. 69; 45; (2013); p. 9481 – 9493;,
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, 4-DMAP (414.4 mg, 3.4 mmol) and di-tert-butyl dicarbonate (740.3 mg, 3.4 mmol) were added to 5-nitro- l //-indole (500.0 mg, 3.1 mmol) in DCM (5 mL), stirred for 1 h at ambient temperature, 2 M HCL was added followed by extraction with DCM, organic phase was collected and the solvent was removed un- der reduced pressure. Yield 724.0 mg (89%). HPLC 100%. LC-MS 263 (M+H)+.

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

Reference£º
Patent; BIOVITRUM AB (PUBL); WO2007/147874; (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.1075-35-0,5-Chloro-2-methylindole,as a common compound, the synthetic route is as follows.

General procedure: Para substituted chalcones (1 equiv.) (9-16) and malononitrile (1equiv.) were stirred in acetonitrile in the presence of L-proline catalyst at room temperature for half an hour. To this reaction mixture different 2-methyl indole (0.8 equiv.) were added and was heated to 90 C on an oil bath. Reaction mixture was stirred till the completion of reaction as monitored by TLC. Afterwards, the reaction mixture was evaporated to dryness under vacumm and was partitioned between ethyl acetate and water. The combined organiclayer was dried and purified by silica gel column chromatographyto get pure products 17-29 [50]., 1075-35-0

1075-35-0 5-Chloro-2-methylindole 70636, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Gupta, Sampa; Maurya, Pooja; Upadhyay, Akanksha; Kushwaha, Pragati; Krishna, Shagun; Siddiqi, Mohammad Imran; Sashidhara, Koneni V.; Banerjee, Dibyendu; European Journal of Medicinal Chemistry; vol. 143; (2018); p. 1981 – 1996;,
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

133831-28-4, Methyl 3-Formylindole-6-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Sodium methoxide (1 g, 0.018 mol) was added in one portion to a mixture of 2-diethylphosphonyl-2H-1,4-benzoxazin-3(4H)-one (3.42 g, 0.012 mol) and 6-methoxycarbonylindol-3-carboxaldehyde (2.55 g, 0.012 mol) in methanol (60 ml). The reaction mixture was refluxed for 21 h, then cooled at room temperature and the precipitated solid was collected by filtration, washed with methanol and dried. Yield 2.78 g (87%) as a mixture of isomers., 133831-28-4

As the paragraph descriping shows that 133831-28-4 is playing an increasingly important role.

Reference£º
Patent; Abbott GmbH & Co. KG; US7049312; (2006); 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

50820-65-0, Methyl 1H-indole-6-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,50820-65-0

Example 1; Preparation of (2E)-3-{4-[({1-[({3-CycIohexyl -1-[2- (dimethylamino) – 2-oxoethyl -2-phenyl-1H-indol-6-yl}carbonyl)amino]cyclopenthyl}carbonyl) amino]phenyl }acrylic acid; Step 1; 3-Cyclohex-1-en-1-yl-1H-indole-6-carboxylic acid; To a solution of methyl-indole-6-carbochiylate in MeOH (1,7 M) was added cyclohexanone (3.0eq.) followed by 30percent NaOMe in MeOH (6,0 eq.) in 100 ml portions over 20 min. The resulting mixture was stirred at RT for 45 min and relaxed for 8 h. Water was added, and the mixture stirred at RT until all solids had dissolved. The organic solvent was removed under vacuum and the pH of the aqueous phase adjusted to 1, by slow addition of concentrated HCl at 0 ¡ãC. The precipitate was isolated by filtration, and then washed with water, until the pH of the water reached 6- 7, Drying under high vacuum gave the title compound as a beige solid (100percent),

The synthetic route of 50820-65-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI SPA; WO2006/29912; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.933-67-5,7-Methyl-1H-indole,as a common compound, the synthetic route is as follows.

General procedure: A 50 mL round bottom flask equipped with a magnetic stirring bar was charged with substituted indole 1 (1.0 mmol, 1.0 equiv), HMTA (2.0 mmol, 0.2803 g, 2.0 equiv), activated carbon (0.1 g) and DMF (2 mL). Then I2 (0.2 mmol, 0.0507g, 20 mol%) was added and the flask was equipped with a reflux condenser. The reaction mixture was stirred at 120 oC under open air and monitored by TLC. Upon completion of the reaction, the reaction mixture was cooled to room temperature. The resultant mixture was filtered through a pad of celite and the filter cake was washed thoroughly with EtOAc (4 ¡Á 6 mL). The filtrate was washed with 0.5 M aqueous HCl (10 mL), saturated NaHCO3 solution (10 mL) and saturated NaCl solution ( 10 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by flash column chromatography on silica gel eluted with hexane and ethyl acetate to give the product., 933-67-5

933-67-5 7-Methyl-1H-indole 70275, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Wang, Qing-Dong; Yang, Jin-Ming; Fang, Dong; Ren, Jiangmeng; Zeng, Bu-Bing; Tetrahedron Letters; vol. 58; 30; (2017); p. 2877 – 2880;,
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.614-96-0,5-Methylindole,as a common compound, the synthetic route is as follows.,614-96-0

Example 3; 1. Synthesis of 3-cyanoindole derivatives with a terminal carboxylic acid; A basic synthetic method of a derivative with a terminal carboxylic acid is shown in the following scheme. [Show Image] An objective compound was prepared by (1) formylation of 3-position of the corresponding indole using phosphorus oxychloride in the presence of dimethylformamide (Vilsmeier method), (2) cyanation by dehydrating reaction with hydroxylamine in sodium formate and formic acid, (3) coupling with ethyl 4-fluorobenzoate in the presence of potassium fluoride on almina and 18-crown-5-ether in dimethylsulfoxide and then, (4) hydrolysis with lithium hydroxide in total 4 steps in that order. The results are shown in the following Table 1. In addition, XO-CH146 (R=H) was prepared from the third step using 3-cyanoindole purchased.; 1. Synthesis of XO-CH164 XO-CH155; Under an argon atmosphere, 5-methyl indole (1.04 g, 7.93 mmol) was dissolved in dimethylformamide (10 mL), and to the solution was added dropwise phosphorus oxychloride (2mL) under ice-cooling, and the resulting mixture was stirred for 1.5 hours at room temperature. To the reaction mixture was added dropwise an aqueous sodium hydroxide solution (5 g/15 mL) under ice-cooling, and the mixture was heated for reflux for an hour. The reaction mixture was adjusted to pH2 to 3 with concentrated hydrochloric acid under ice-cooling, and then, the solid was collected by filtration and dried at 60C under reduced pressure to give XO-CH155 as a pale pink solid (1.13 g, 90% yield).

The synthetic route of 614-96-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Kissei Pharmaceutical Co., Ltd.; EP1932833; (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

4771-49-7, 6-Methylindole-3-carboxyaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,4771-49-7

EXAMPLE 129 3-(6-Methylindol-3-yl)-2-[(2R),(3S)-2,3,4-trihydroxy-butylthio]-1-(3,4,5-trimethoxyphenyl)-2-propen-1-one (Compound 129) 3′,4′,5′-Trimethoxy-2-[(2R),(3S)-2,3,4-trihydroxy-butylthio]acetophenone (1.73 g) obtained in Reference Example 23 and 6-methylindole-3-carbaldehyde (0.80 g) were dissolved in ethanol (10 ml), and piperidine (0.43g) was added thereto, followed by heating under reflux for 48 hours. The reaction solution was concentrated under reduced pressure and the residue was purified by silica gel column chromatography. The obtained crude crystals were recrystallized from a mixed solvent of ethyl acetate and hexane to give Compound 129 (1.12 g). 1 H-NMR (270 MHz, CDCl3) delta2.43 (s, 3H), 2.95 (dd, J=13.6, 8.7 Hz, 1H), 3.10 (dd, J=13.6, 4.0 Hz, 1H), 3.17 (brs, 1H), 3.53 (d, J=6.3 Hz, 1H), 3.64-3.82 (m, 4H), 3.84 (s, 6H), 3.96 (s, 3H), 4.83 (d, J=4.0 Hz, 1H), 7.01 (d, J=8.2 Hz, 1H), 7.07 (s, 2H), 7.20 (s, 1H), 7.37 (d, J=8.2 Hz, 1H), 7.97 (s, 1H), 8.59 (d, J 2.6 Hz, 1H), 9.36 (brs, 1H) FAB-MS m/z=488 (M+ +1) Elemental Analysis: C25 H29 NO7 S Calcd.(percent): C, 61.59; H, 6.00; N, 2.87 Found (percent): C, 61.56; H, 6.14; N, 2.82

As the paragraph descriping shows that 4771-49-7 is playing an increasingly important role.

Reference£º
Patent; Kyowa Hakko Kogyo Co., Ltd.; US5952355; (1999); 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