Day: September 16, 2020

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 5-azaindole (5.00 g) and Et3N (12 mL) was added (Boc)20 ( 14 mL) dropwise at 0C. The mixture was stirred for 6 h, then diluted with water and extracted with EtOAc. The organic layer was dried over Na2S04 for 1 h and filtered. The filtrate was concentrated in vacuo and the residue was chromatographed with a silica gel column (eluting agent: 3: 1 (v/v) PE/EA) to give the title compound as transparent liquid (9.00 g, 97.00 %). The compound was characterized by the following spectroscopic data: ? NMR (400 MHz, CDC13) ?: 1.65 (s, 9H), 6.62 (d, J = 3.6 Hz, 1H), 7.25 (d, J = 5.3 Hz, 1 H), 7.50 (d, J = 3.5 Hz, 1H), 8.42 (d, J= 5.3 Hz, 1 H), 9.43 (s, lH) ppm., 271-34-1

The synthetic route of 271-34-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Jiancun; ZHANG, Yingjun; ZHANG, Weihong; LIU, Bing; ZHANG, Jiquan; LIU, Jinlei; ZHANG, Lu; WO2013/71697; (2013); 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

399-76-8, 5-Fluoroindole-2-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5-Fluorondole-2-carboxylic acid (5.00g, 27.91mmol) was added to ethanol (50mL) at 0 ¡ãC. SOCl2 (9.84g, 82.71mmol) was added to the mixture and the reaction mixture was warmed to reflux and stirred for 5 hours. TLC showed the reaction was complete, the reaction mixture was concentrated, and saturated aqueous NaHCO3 solution (15mL) was added thereto. The resulting mixture was extracted with DCM (100mL * 2) and the organic phase was dried over anhydrous sodium sulfate and concentrated to deliver the title compound (light yellow solid, 5.50g, yield 85.60percent). 1H-NMR (400 MHz, CDCl3) delta 9.00 (br. s., 1 H), 7.31 – 7.39 (m, 2 H), 7.19 (d, J=1.2Hz, 1 H), 7.10 (td, J=9.0, 2.4 Hz, 1 H), 4.43 (q, J=7.1 Hz, 2 H), 1.43 (t, J=7.1 Hz, 3 H)., 399-76-8

399-76-8 5-Fluoroindole-2-carboxylic acid 1820, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; GUANGDONG ZHONGSHENG PHARMACEUTICAL CO., LTD; DING, Charles Z.; CHEN, Shuhui; ZHAO, Baoping; LIU, Xile; XIAO, Linxia; DING, Chao; WANG, Fei; LI, Jian; (153 pag.)EP3290419; (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

172595-68-5, Methyl 5-methoxy-1H-indole-3-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

172595-68-5, Methyl 5-methoxy-1H-indole-3-carboxylate (200 mg, 0.97 mmol) used hydrolysis reaction (2 NNaOH water solution) to aord DX-01-06 (white solid, 140 mg, yield 75%). 1H-NMR (400 MHz,CD3OD): = 7.88 (s, 1H, H-indolyl), 7.57 (d, J = 2.4 Hz, 1H, H-indolyl), 7.31 (d, J = 8.8 Hz, 1H,H-indolyl), 6.83 (dd, J = 8.8, 2.5 Hz, 1H, H-indolyl), 3.83 (s, 3H, CH3). 13C-NMR (101 MHz, CD3OD): = 156.99, 133.58, 128.36, 115.37, 114.23, 113.88, 113.61, 104.51, 103.64, 56.06. HRMS (ESI): m/z [M + H]+calculated for C10H10NO3: 192.06552; found: 192.06645.

As the paragraph descriping shows that 172595-68-5 is playing an increasingly important role.

Reference£º
Article; Wen, Hui; Liu, Yuke; Wang, Shufang; Wang, Ting; Zhang, Gang; Chen, Xiaoguang; Li, Yan; Cui, Huaqing; Lai, Fangfang; Sheng, Li; Molecules; vol. 24; 11; (2019);,
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

1074-86-8, 1H-Indole-4-carbaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

K2CO3 (19.2 g, 138.93 mmol) and 2-fluorobenzonitrile (9.18 g, 75.87 mmol) were added to a solution of 24 (10 g, 68.97 mmol) in 100 mL DMF. The mixture was stirred and refluxed for 1 h. After cooling to rt, the mixture was added to 100 mL water and extracted with ethyl acetate (100 mL * 3). After that the organic phase was collected and washed with NaCl saturated solution (150 mL * 5) and then dried over MgSO4. After filtration, the solvent was removed under reduced pressure. The residue was recrystallized by ethyl acetate to obtain white solid. Yield: 89.1percent. MP: 240-243 ¡ãC. 1H NMR (400 MHz, CDCl3) delta: 10.32 (s, 1H), 7.91 (d, 1H), 7.81 (t, 1H), 7.76 (d, 1H), 7.61-7.56 (m, 5H), 7.42 (t, 1H). MS (ESI): [M + H]+ calcd 247.1; found 247.2.

1074-86-8, As the paragraph descriping shows that 1074-86-8 is playing an increasingly important role.

Reference£º
Article; Zhu, Weibo; Bao, Xiaolu; Ren, He; Da, Yajing; Wu, Dan; Li, Fuming; Yan, Yijia; Wang, Li; Chen, Zhilong; European Journal of Medicinal Chemistry; vol. 115; (2016); p. 161 – 178;,
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

247564-66-5, 4,6-Difluoroindole-2-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of the above compound (3.0 g) and copper powder (2.9 g) in quinoline (30 ml) was stirred at 200 C. for 5 hours under argon atmosphere. After being cooled to room temperature, the insoluble materials were filtered off and washed with ethyl acetate (100 ml). The filtrate was washed with a 6 N aqueous hydrochloric acid solution twice and brine. The each aqueous layer was extracted with ethyl acetate, and the combined organic layer was dried over magnesium sulfate and treated with activated carbon. The insoluble materials were filtered off, and the filtrate was evaporated under reduced pressure. The residual oil was purified by silica gel column chromatography (hexane:ethyl acetate=10:1-6:1) to give 4,6-difluoroindole (2.60 g) as pale yellow oil. ESI-Mass m/Z 152 (M-H).

247564-66-5, 247564-66-5 4,6-Difluoroindole-2-carboxylic acid 3451441, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Tanabe Seiyaku Co., Ltd.; US2008/27122; (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

487-89-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.487-89-8,Indole-3-carboxaldehyde,as a common compound, the synthetic route is as follows.

General procedure: To a dry dichloromethane solution (10 mL) of the appropriate 1H-indole-3-carbaldehydes(2 mmol), anhydrous potassium carbonate (6 mmol) and benzenesulfonyl chlorides (4 mmol) indry dichloromethane (20 mL) were added, and the mixture was stirred for 12 h at 40 C. After thecompletion of the reaction, excess solvent was removed under reduced pressure to obtain a yellowcrude solid of 3a-3b which was directly used in the next step without purification.

487-89-8 Indole-3-carboxaldehyde 10256, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Song, Ming-Xia; Li, Song-Hui; Peng, Jiao-Yang; Guo, Ting-Ting; Xu, Wen-Hui; Xiong, Shao-Feng; Deng, Xian-Qing; Molecules; vol. 22; 6; (2017);,
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

103858-53-3, Ethyl 6-bromoindole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reference Example 61 A mixture of ethyl 6-bromo-1H-indole-2-carboxylate (2.5 g) and 4-methylphenylboric acid (1.39 g), potassium carbonate (2.58 g) and toluene/ethanol/water (90/9/9 ml) was stirred at room temperature for one hour. Into the reaction mixture was added tetrakis(triphenylphosphine)palladium (0.32 g), and the resulting mixture was heated at reflux for 18 hours. After cooling to room temperature, the mixture was extracted with ethyl acetate. The organic layer was washed with an aqueous saturated solution of sodium chloride and was dried with magnesium sulfate. After concentration under reduced pressure, the residue was subjected to purification using column chromatography (ethyl acetate/hexane 1:5?1:2?1:1) and to recrystallization (ethyl acetate/hexane) to obtain ethyl 6-(4-methylphenyl)-1H-indole-2-carboxylate (1.92 g) as colorless crystals.

103858-53-3, The synthetic route of 103858-53-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Takeda Chemical Industries, Ltd.; US6627651; (2003); 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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.16732-70-0,Ethyl 5-bromo-1H-indole-2-carboxylate,as a common compound, the synthetic route is as follows.

a) 5-Pyridin-3-yl-lH-indole-2-carboxylic acid ethyl ester 5-Bromo-lH-indole-2-carboxylic acid ethyl ester (5.0 g), 3-tributylstannylpyridine (7.552 g), and bis-(triphenylphosphin)-palladium(II)-dichlorid (0.131 mg) were suspended in dioxane (10 mL) and refluxed at 120C overnight. Still starting material left, another bis-(triphenylphosphin)- palladium(II)-dichlorid (0.131 mg) was added, reaction was refluxed over the weekend. The reaction mixture was evaporated, the residue was purified by column chromatography on basic silica gel using heptane / ethyl acetate (7:3) and crystallized in diethylether to yield the title compound as a white solid (1.454 g, 29 %). MS ISP (m/e): 267.1 (100) [(M+H)+].

16732-70-0, 16732-70-0 Ethyl 5-bromo-1H-indole-2-carboxylate 259091, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; BAUMANN, Karlheinz; FLOHR, Alexander; JOLIDON, Synese; KNUST, Henner; LUEBBERS, Thomas; NETTEKOVEN, Matthias; WO2014/60386; (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

1015460-59-9, 7-Bromo-5H-pyrido[4,3-b]indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1015460-59-9, To a solution of custom made 7-bromo-5H-pyrido[4,3-?>]indole (0.49 g, 1.98 mmol) in Lambda/,Lambda/’- dimethylformamide (5 mL) was added cesium carbonate (0.32 g, 0.99 mmol) and the mixture was stirred at room temperature for 10 minutes and dimethylcarbonate was added dropwise (334 mu, 3.96 mmol). The reaction mixture was heated at 160C for 3 hours and after cooling, water (20 mL) and ethyl acetate (20 mL) were added to the mixture. The phases were separated and the aqueous phase was extracted with ethyl acetate (2 X 20 mL). The organic phases were combined and dried over Na2S04. The solvent was removed under reduced pressure and the residue was purified on a HP-Sil column using a Biotage Isolera One purification system employing a dichloromethane/methanol gradient (100/0 -> 90/10) to afford the crude title compound (0.36 g, 69 %). 1H NMR (400 MHz, DMSO-cf6) delta = 9.36 (s, 1 H), 8.52 (d, 1 H), 8.21 (d, 1 H), 7.95 (d, 1 H), 7.62 (d, 1 H), 7.45 (dd, 1 H), 3.88 (s, 3H) MS (ESI): m/z = 263.95 [M+H]+

The synthetic route of 1015460-59-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AC IMMUNE SA; PIRAMAL IMAGING SA; KROTH, Heiko; NAMPALLY, Sreenivasachary; MOLETTE, Jerome; GABELLIERI, Emanuele; BENDERITTER, Pascal, Andre, Rene; FROESTL, Wolfgang; SCHIEFERSTEIN, Hanno; MUELLER, Andre; SCHMITT-WILLICH, Heribert; BERNDT, Mathias; WO2015/110263; (2015); 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

10406-06-1, 5-Bromo-1H-indole-3-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5-bromo-1 H-indole-3-carboxylic acid (3.26 g, 13.6 mmol) was dissolved in dioxane (30 mL). The mixture was purged with nitrogen and cooled to 0-5C. Sodium Hydride (60% in mineral oil) (1 .63 g, 40.8 mmol) was added portionwise over approx. 30 mm under a flow of N2. Gas evolution was observed upon addition. When the addition was completed the mixture was stirred for 30 mm at 0-5C. p-Toluenesulfonyl chloride (5.17 g, 27.1 mmol) was dissolved in dioxane (10 mL) and added dropwise over 1 h to the suspension. The reaction mixturewas allowed to warm up to rt and stirred at temperature overnight. A white insoluble solid was formed. 1 M HCI was added up to pH = 6. The reaction mixture was filtered and washed with CH2CI2. The combined organic layer were washed with brine, dried over Mg504, filtered and the solution was concentrated under reduced pressure. The crude material was purified by flash column chromatography on silica gel with a gradient of CH2CI2/CH2CI2:MeOH (9:1) from [100:0] to [0:100]. The column fractions were concentrated to dryness to afford 5-bromo-1-tosyl-1 H-indole-3-carboxylic acid Ex.65a (1.47 g, 27%) as pale orange solid., 10406-06-1

10406-06-1 5-Bromo-1H-indole-3-carboxylic acid 7018243, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; GENFIT; DELHOMEL, Jean-Francois; PERSPICACE, Enrico; MAJD, Zouher; PARROCHE, Peggy; WALCZAK, Robert; (284 pag.)WO2018/138362; (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