Day: August 26, 2020

1196-70-9, 1H-Indole-6-carbaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 3. Synthesis of (E)-N?-(( 1 H-indol-6-yl)methylene)-2-(2,6-dimethyl-4-(tetrahydrofuran-3 – yl)phenoxy)acetohydrazide: 2-(2,6-dimethyl-4-(tetrahydrofuran-3 -yl)phenoxy)acetohydrazide(30 mg, 0.11 mmol) and 1 H-indol-6-carbaldehyde (17 mg, 0.11 mmol) were dissolved in EtOH1 mL, followed by stirring at 90 C for 3 hours. After the completion of the reaction, the reaction mixture was concentrated under reduced pressure, and purified by column chromatography (hexane:ethyl acetate = 1:1) to obtain Compound 323 (15 mg, 34 %). ?H NMR (400 MHz, DMSO-d6): 611.42-11.39 (m, 1H), 11.37-11.32 (m, 1H), 8.47-8.03 (s, 1H),7.57-7.48 (m, 2H), 7.40-7.37 (m, 2H), 6.95 (m, 2H), 6.47 (m, 1H), 4.74 (s, 1H), 4.31 (s, 1H),3.96 (m, 3H), 3.75 (m, 2H), 2.32 (s, 3H), 2.21 (s, 3H).

1196-70-9 1H-Indole-6-carbaldehyde 2773435, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; INJE UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION; CHOI, HoJin; LEE, JaeWon; LEE, ChangGon; HA, NiNa; SEO, Su Kil; LEE, SunMi; LEE, Song-Min; WO2014/35149; (2014); 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.252061-66-8,5-Hydroxyisoindolin-1-one,as a common compound, the synthetic route is as follows.

B17: 5-(4-Chloro-butoxy)-2,3-dihydro-isoindol-1 -oneTo a suspension of 5-Hydroxy-2,3-dihydro-isoindol-1-one (2.03 g, 13.6 mmol) in acetonitrile (17 mL) was added 1-bromo-4-chloro-butane (5.65 g, 32.9 mmol), potassium carbonate (4.63 g, 33.5 mmol), and potassium iodide (0.70 g, 0.31 mmol). After heating at reflux for 18 h the mixture was concentrated and crystallized from acetonitrile/water to obtain 5-(4-Chloro-butoxy)-2,3-dihydro-isoindol-1-one (B17), <3.23 g, 98 %). MS: ES: M+1 : 240.0 (239.6) The synthetic route of 252061-66-8 has been constantly updated, and we look forward to future research findings. Reference£º
Patent; PFIZER PRODUCTS INC.; WO2008/20306; (2008); 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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.35320-67-3,2-Methyl-1H-indol-4-ol,as a common compound, the synthetic route is as follows.

To a stirred solution of 2-chloro-N-[(3- fluorophenyl)methyl] -7,8-dihydro-5H-pyrano [4,3-d]pyrimidin-4-amine (350 mg, 1.19 mmol) in Dioxane (20 ml) were added 2-methyl-1H-indol-4-ol (193 mg, 1.31 mmol), Pd2dba3 (218 mg, 0.24 mmol), X-Phos (113 mg, 0.24 mmol) and Cs2CO3 (782 mg, 2.38 mmol). The black suspension was stirred at 100 oC for 3 h under N2. TLC showed the reaction was completed. The reaction was filtered through a pad of celite and the filtrate was diluted with EtOAc (50 mL) and H2O (20 mL). The aqueous layer was extracted with EtOAc (20 mL x 3), dried over Na2SO4 and concentrated in vacuo. The red oil was purified via silica gel column chromatography (hexane and ethyl acetate) to afford the desired product 1-(4-((3-fluorobenzyl)amino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin- 2-yl)-2-methyl-1H-indol-4-ol (300 mg, 54%) as a yellow solid.

As the paragraph descriping shows that 35320-67-3 is playing an increasingly important role.

Reference£º
Patent; CLEAVE BIOSCIENCES, INC.; ZHOU, Han-Jie; WUSTROW, David; (498 pag.)WO2016/200840; (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.53330-94-2,1-(1H-Indol-5-yl)ethanone,as a common compound, the synthetic route is as follows.

To a solution of 24 (500 mg, 3.14 mmol) in 20 mL anhydrous THF,NaH (60%, 188 mg, 4.71 mmol) was added and the mixture wasstirred for 15 min. Then, (Boc)2O (822 mg, 4.71 mmol) was addeddropwise. After stirring for 1 h, the mixture was diluted with 50 mLEtOAc, then washed with water (20 mL x 3), saturated brine, driedover anhydrous Na2SO4, and concentrated in vacuo to afford thecrude product, which was purified by column chromatographywith petroleum/ethyl acetate (5:1) to give intermediate 21a(650 mg, 79.9%). The spectral data of 21c was in accordance withliterature report [36].

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

Reference£º
Article; Li, Wenlong; Shuai, Wen; Sun, Honghao; Xu, Feijie; Bi, Yi; Xu, Jinyi; Ma, Cong; Yao, Hequan; Zhu, Zheying; Xu, Shengtao; European Journal of Medicinal Chemistry; vol. 163; (2019); p. 428 – 442;,
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

1477-50-5, 1H-Indole-2-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: H2SO4 (98%) (0.5mL) was added to a stirred solution of raw material1 in CH3OH (10mL) at room temperature and the mixture was then stirred for 2-3 h at 80 C. TLC was used to monitor the reaction progress until it was complete. A large amount of ice water was then added to the mixture. A saturated solution of sodium carbonate was used to neutralise the mixture until white solid appeared. After filtering the mixed solution, compounds 2a-h (yield 91-99) were obtained.

The synthetic route of 1477-50-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Ye, Ying; Suo, Yourui; Yang, Fang; Yang, Yongjing; Han, Lijuan; Journal of Chemical Research; vol. 39; 5; (2015); p. 296 – 299;,
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.143612-79-7,3-(4-Chlorobutyl)-1H-indole-5-carbonitrile,as a common compound, the synthetic route is as follows.

General procedure: A mixture of 3-(4-chlorobutyl)-1H-indole-5-carbonitrile (6a,116 mg, 0.5 mmol), corresponding intermediates 7e (0.5 mmol)and KI (0.05 mmol) was added Et3N (1 mmol). The reaction mixturewas stirred at reflux temperature for 24 h. Then removal thesolvent under vacuum and the residue was purified by columnchromatography (CH3OH:CH2Cl2 = 1:20 to 1:10, v:v) to afford compound2a. Compound 2a was isolated as a yellow powder, 40%yield.

As the paragraph descriping shows that 143612-79-7 is playing an increasingly important role.

Reference£º
Article; Liu, Wenwen; Wang, Huan; Li, Xiaokang; Xu, Yixiang; Zhang, Jian; Wang, Wei; Gong, Qi; Qiu, Xiaoxia; Zhu, Jin; Mao, Fei; Zhang, Haiyan; Li, Jian; Bioorganic and Medicinal Chemistry; vol. 26; 12; (2018); p. 3117 – 3125;,
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.57476-50-3,1-Boc-3-Formylindole,as a common compound, the synthetic route is as follows.

STR51 2-(N-Boc-3-Indolyl)-4-quinolinecarboxylic Acid To a 500 mL round bottom flask was added 27.2 g (0.31 mol) of pyruvic acid (Lancaster), N-Boc-indole-3-carboxaldehyde (0.16 mol) and 200 mL of acetic acid. The reaction mixture was heated at 85 C. until all the solid material had dissolved (~30 min). Then aniline (0.31 mol) was added and the reaction mixture was stirred for 90 minutes at 85 C. The precipitate was filtered hot in a fritted funnel and washed with acetic acid (2*50 mL) and then with ether (2*50 mL). The solid filter cake was dried in vacuo to yield 2-(N-Boc-3-indolyl)-4-quinolinecarboxylic Acid (3-50% yield) of pure (>95%) material.

As the paragraph descriping shows that 57476-50-3 is playing an increasingly important role.

Reference£º
Patent; Sepracor, Inc.; US6103905; (2000); 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

90923-75-4, 1-Methyl-1H-indole-5-carbaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a solution of AB-region starting material (1.0 equiv) in THF was added dropwise 2.5 M n-BuLi solution in n-hexane (1.05 equiv) at -78 C. The reaction mixture was stirred for 10 min at -78 C, and DE-region aldehyde (1.0 equiv) was added. The reaction mixture was stirred for an additional 30 min and was warmed to ambient temperature. The reaction mixture was quenched with saturated NH4Cl solution and extracted with EtOAc. The organic layer was washed with brine, dried over MgSO4, and concentrated under reduced pressure. The residue was purified by flash column chromatography on silica gel to afford the corresponding compound.

90923-75-4 1-Methyl-1H-indole-5-carbaldehyde 7537534, aindole-building-block compound, is more and more widely used in various.

Reference£º
Article; Kim, Ho Shin; Hong, Mannkyu; Ann, Jihyae; Yoon, Suyoung; Nguyen, Cong-Truong; Lee, Su-Chan; Lee, Ho-Young; Suh, Young-Ger; Seo, Ji Hae; Choi, Hoon; Kim, Jun Yong; Kim, Kyu-Won; Kim, Joohwan; Kim, Young-Myeong; Park, So-Jung; Park, Hyun-Ju; Lee, Jeewoo; Bioorganic and Medicinal Chemistry; vol. 24; 22; (2016); p. 6082 – 6093;,
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

1670-83-3, Indole-7-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 19; Preparation of 1H-Indole-7-carboxylic acid (4-tert-butyl-benzyl)-[2-(2,6-dichloro-phenyl)-ethyl]-amide; To a solution of 48 mg (0.3 mmol) of 1H-indole-7-carboxylic acid and 96 mg of TBTU (0.3 mmol) in 4 ml DMF, were added 0.26 ml (1.5 mmol) of N,N-diisopropylethyl amine. After stirring for 5 min at rt, 106 mg (0.3 mmol) (4-tert-butyl-benzyl)-[2-(2,6-dichloro-phenyl)-ethyl]-amine in 1 ml DMF was added. After stirring for 2 h at rt, the reaction mixture was diluted with 50 ml water and extracted with 2¡Á50 ml EtOAc. The combined organic phases were washed with water and brine, dried with magnesium sulfate, filtered and concentrated in vacuo. The residue was crystallized from diethylether, leading to 123 mg white solid (85%). MS (ISP) 479.5 (M+H)+.

As the paragraph descriping shows that 1670-83-3 is playing an increasingly important role.

Reference£º
Patent; Conte-Mayweg, Aurelia; Kuehne, Holger; Luebbers, Thomas; Maugeais, Cyrille; Mueller, Werner; Pflieger, Philippe; US2006/30613; (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.128742-76-7,Methyl 1-methyl-1H-indole-5-carboxylate,as a common compound, the synthetic route is as follows.

A solution of l-methyl-l//’-indole-5-carboxylic acid methyl ester (0.38 g, 2.0 mmol), prepared using procedures as described in Example 1, Ag?O (0.51 g, 2.2 mmol), 4-nitro-benzyl bromide (0.48 g, 2.2 mmol) and dioxane (6 mL) was heated to reflux for 25 hr, then more 4-nitro-benzyl bromide (0.48 g, 2.2 mmol) was added and the solution was heated at reflux an additional 4 days. After cooling to room temperature, the reaction mixture was diluted with ether (50 mL) and ethyl acetate (50 mL), washed with aq. NH4Cl (50 mL) and then brine (50 mL). The organic layer was dried over MgSO4, filtered and concentrated. The remaining residue was subjected to flash chromatography (ethyl acetate/hexane, 1:4) to provide of l-methyl-3-(4-nitro-phenylmethyl)-l//-indole- 5-carboxylic acid methyl ester (0.38 g, 58% yield). 1H NMR (400 MHz, CDCl3) delta 8.26 (s, IH), 8.16 (d, 2H, J= 8.3 Hz), 7.98 (d, IH, J= 8.3 Hz), 7.45 (d, 2H, J= 8.3 Hz), 7.35 (d, IH, J= 8.3 Hz), 6.90 (s, IH), 4.25 (s, 2H), 3.94 (s, 3H), 3.82 (s, 3H).

The synthetic route of 128742-76-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PHARMACYCLICS, INC.; WO2007/109178; (2007); 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