Day: October 28, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.830-96-6,3-Indolepropionic acid,as a common compound, the synthetic route is as follows.

To a 10 ml reaction tube by sequentially adding a substrate (0.2 mmol, 37.8 mg), trimethyl twelve alkyl iodide (0.02 mmol, 7.2 mg), 2 ml of water, and finally adding hydrogen peroxide (0.12 mmol, 120 mul). The reaction mixture at 60 C under stirring 48 h after stopping the reaction, to the reaction system by adding ethyl acetate (5 ml * 4), the combined organic phase and drying with anhydrous sodium sulfate, filtered vacuum concentrated to obtain the crude product. The resulting crude product is purified by column chromatography separation, to obtain white solid product, separating the yield is 67%

830-96-6, The synthetic route of 830-96-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Huazhong University of Science and Technology; Zhong Fangrui; Wang Dangui; (18 pag.)CN109776381; (2019); 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.16732-57-3,Ethyl 5-nitro-1H-indole-2-carboxylate,as a common compound, the synthetic route is as follows.

5-Nitro-1 H-indole-2-carboxylic acid ethyl ester (14.9 mmol) was suspended in acetone(50 ml) and added to a mixture of titanium(lll) chloride (91ml, >10% in 2M hydrochloric acid) and ammonium acetate (265ml, 4M). The reaction was stirred for 2h and neutralized with saturated sodium hydrogen carbonate. The mixture was extracted with ethyl acetate (100ml) and the organic layer dried (MgSO4). The solvent was removed in vacuo to give a light brown solid which was purified by silica chromatography to give the title compound as an off-white solid (1.57g) m/z = 205 in MS ES+.

16732-57-3, As the paragraph descriping shows that 16732-57-3 is playing an increasingly important role.

Reference£º
Patent; MEDIVIR AB; WO2007/6714; (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

16732-80-2, Ethyl 4-methyl-1H-indole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

d) Synthesis of ethyl 1-[(2-ethoxycarbonylmethoxy)ethyl]-4-methyl-1H-indole-2-carboxylate A solution of ethyl [2-(toluene-4-sulfonyloxy)ethoxy]acetate (3.90 g, 12.9 mmol) in N,N-dimethylformamide (10 ml) was added dropwise to a mixture of ethyl 4-methyl-1H-indole-2-carboxylate (2.50 g, 12.3 mmol), 60% sodium hydride (0.50 g, 12.5 mmol) and N,N-dimethylformamide (45 ml) at room temperature, and the resulting mixture was stirred at room temperature 7 hours. The reaction mixture was poured into a 10% aqueous sodium chloride solution and extracted with ethyl acetate, and the extract solution was washed with a 5% aqueous sodium chloride solution and dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure and the resulting residue was purified by a silica gel column chromatography (eluent:ethyl acetate:n-hexane= 2:98) to obtain 1.86 g of ethyl 1-[(2-ethoxycarbonylmethoxy)ethyl]-4-methyl-1H-indole-2-carboxylate as a colorless oil. 1 Hnmr (CDCl3) delta: 1.23(3H, t, J=7.3 Hz), 1.42(3H, t, J=7.3 Hz), 2.55(3H, s), 3.91(2H, t, J=5.9 Hz), 3.98 (2H, s), 4.16(2H, q, J=7.3 Hz), 4.37(2H, q, J=7.3 Hz), 4.78(2H, t, J=5.9 Hz), 6.94(1H, d, J=6.9 Hz), 7.24(1H, dd, J=6.9, 6.9 Hz), 7.35(1H, s), 7.36(1H, d, J=6.9 Hz).

16732-80-2, The synthetic route of 16732-80-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sumitomo Pharmaceuticals Company, Limited; US5834454; (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

15861-24-2, Indole-5-carbonitrile is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: NaN3 (0.975 g, 15 mmol) was dissolved in DES (10 mL) at room temperature by stirring until a clear solution was formed. Then benzonitrile (10 mmol) was added. The reaction mixture was constantly stirred at 140 C and monitored by TLC. After completion of the reaction, the reaction mixture was cooled to room temperature and poured into the cold water (10 mL). The solid was obtained and filtered. The obtained solid is taken into cold water (10 mL). Then it was acidified carefully to pH 5 with 5 M HCl. The organic material was extracted thrice with ethyl acetate; the resultant organic layer was washed with distilled water, dried over anhydrous sodium sulfate, and concentrated to give the crude solid crystalline 5-substituted 1H-tetrazole. The resulting product, although evident as a single compound by TLC, was purified by simple recrystallization from aqueous ethanol giving pure 5-substituted 1H-tetrazoles.

15861-24-2, The synthetic route of 15861-24-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Padvi, Swapnil A.; Dalal, Dipak S.; Synthetic Communications; vol. 47; 8; (2017); p. 779 – 787;,
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, Part F. 5-Nitro-1H-indole (2.5 g, 15 mmol), di-tert-butyl dicarbonate (3.6 g, 17 mmol), and DMAP (190 mg, 1.5 mmol) were dissolved in 150 mL of THF. The solution was stirred for 12 h at rt under N2 and was then concentrated. The residue was taken up in EtOAc and the mixture was filtered. The filtered solid was washed with 100 mL of hexanes and dried to give tert-butyl-5-nitro-1H-indole-1-carboxylate as an off-white solid (3.1 g, 78%). LRMS (AP+): 304.2 (M+H+ACN)+. 1H NMR (CDCl3) delta 8.51 (d, 1H), 8.23-8.29 (m, 2H), 7.75 (d, 1H), 6.73 (d, 1H), 1.71 (s, 9H).

6146-52-7 5-Nitroindole 22523, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Bristol-Myers Squibb Company; Pinto, Donald J.P.; Quan, Mimi L.; Orwat, Michael J.; Li, Yun-Long; Han, Wei; Qiao, Jennifer X.; Lam, Patrick Y.S.; Koch, Stephanie L.; (132 pag.)US2017/50964; (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.1196-70-9,1H-Indole-6-carbaldehyde,as a common compound, the synthetic route is as follows.

General procedure: To a solution of 5 (0.2 mmol) in anhydrous THF, NaH (60%,0.24 mmol) was added at 0 C under N2 atmosphere. After stirring for15 min, aromatic aldehyde (0.24 mmol) was added into the mixture andthe reaction was stirred for another 1 h. The reaction mixture was thenextracted with EtOAc (3¡Á20 mL). The combined organic layers werethen washed with saturated brine, dried over anhydrous Na2SO4, andconcentrated in vacuo. The residue was purified by flash columnchromatography using PE/EA (5/1, V/V) as an eluent to afford thecompounds 7a-n, 8a-d.

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

Reference£º
Article; Li, Wenlong; Sun, Honghao; Xu, Feijie; Shuai, Wen; Liu, Jie; Xu, Shengtao; Yao, Hequan; Ma, Cong; Zhu, Zheying; Xu, Jinyi; Bioorganic Chemistry; vol. 85; (2019); p. 49 – 59;,
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 27; Preparation of 1H-Indole-7-carboxylic acid (4-tert-butyl-benzyl)-[2-(2-fluoro-3-trifluoromethyl-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 3 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) of (4-tert-butyl-benzyl)-[2-(2-fluoro-3-trifluoromethyl-phenyl)-ethyl]-amine in 2 ml DMF were added. After stirring for 4 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 purified by column chromatography (8 g silica gel; EtOAc/heptane 1:6) to give 112 mg light yellow solid (73%). MS (ISP) 497.4 (M+H)+., 1670-83-3

1670-83-3 Indole-7-carboxylic acid 74281, aindole-building-block compound, is more and more widely used in various fields.

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

14805-29-9, exo-Hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 2To the reaction mixture containing Compound (C) which was obtained in the above Example 1 were added (3aR,4S,7R,7aS)-hexahydro-4,7-methano-2H-isoindole-1,3-dione [Compound (D)] (22.6 g, 136.8 mmol), potassium carbonate (15.1 g, 109.3 mmol) and toluene (44 g).Then, the toluene (44 g) was distilled out from the mixture, water (0.82 g) was added thereto, and the resulting mixture was reacted under reflux for 8 hours.Then, the reaction mixture was cooled to room temperature, and water (400 g) was added to the mixture.The mixture was separated with a separating funnel, and the toluene layer was washed with 2.3percent (W/W) brine (350 g).Further, active carbon (1.8 g) was added to the toluene solution, and the mixture was stirred for 1 hour.The active carbon was removed by filtration to give a toluene solution containing (3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl) piperazin-1-ylmethyl]cyclohexylmethyl}hexahydro-4,7-methano-2H-isoindole-1,3-dione (2-[[(1R,2R)-2-[[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]methyl]cyclohexyl]-methyl]hexahydro-(3aS,4R,7S,7aR)-4,7-methano-1H-isoindole-1,3(2H)-dione) [Compound (E)] (341.4 g).The yield of Compound E was 94.3percent The yield of Compound (E) was calculated based on the analytical result that the content of the compound in the toluene solution was 12.4percent (w/w) (which was calculated by LC absolute calibration curve method).And, the production rate of by-product (R) was 0.013percent (which was calculated with the following formula (a))., 14805-29-9

Big data shows that 14805-29-9 is playing an increasingly important role.

Reference£º
Patent; Dainippon Sumitomo Pharma Co., Ltd.; US2011/263848; (2011); 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

244-76-8, 9H-Pyrido[2,3-b]indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2-necked 250ml flask, the compound (4) (0.6g, 1.23mmol), alpha-carboline (0.45g, 2.71mmol), NaOtBu (0.35g, 3.69mmol) were placed in toluene (100ml) was stirred under nitrogen, and the reaction temperature the temperature was raised to 80 C and reacted for 1 hour. To the resulting solution was added Pd (dba) 2 (0.02g, 0.04mmol), (tert-Bu) 3P (0.01g, 0.06mmol) and allowed to react at 80 C for 1 ~ 2days. Remove salts by filtration of the reaction solution It was. Remove the toluene was evaporated from the solution by filtration, remove the concentrate to the column to obtain the compound (3-10, AnT-DaC3) 0.49g (yield: 60%)

244-76-8, The synthetic route of 244-76-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; WS Co., Ltd; Ko, Byung Soo; Kim, Kyu Sik; Oh, Yu Jin; (52 pag.)KR101528768; (2015); 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.18372-22-0,Methyl 2-(1H-indol-3-yl)-2-oxoacetate,as a common compound, the synthetic route is as follows.

In a three-necked flask, 47 mL lithium aluminum hydride (4.44 g, 117 mmol, 2.5 mol/L THF solution) was injected under Nitrogen at 0 C. 10.15 g (50 mmol) 1 was dissolved in 36 mL of dry THF. The above solution was added dropwise for a period of 1 h, then heated to 70 C for 4 hours. The reaction was complete and quenched by the Fisher treatment for a suspension. The suspension was filtered and the filter cake washed with ethyl acetate. The combined organic layer was wash with brine, dry over Na2SO4 and concentrated in vacuum. The residue was purified by flash silica gel column chromatography(ethyl acetate / petroleum ether, 25%) to obtain a white solid 2 (6.44 g, 80% yield)., 18372-22-0

The synthetic route of 18372-22-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Guo, Zhenbo; Xu, Yiming; Peng, Yujie; Haroon ur Rashid; Quan, Wei; Xie, Peng; Wu, Lichuan; Jiang, Jun; Wang, Lisheng; Liu, Xu; Bioorganic and Medicinal Chemistry Letters; vol. 29; 9; (2019); p. 1133 – 1137;,
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