Month: November 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.15317-58-5,1H-Indole-3-carbohydrazide,as a common compound, the synthetic route is as follows.

General procedure: 1H-Indole-3-carboxylate methylester 2 (1.0 mmol-equiv.) was refluxed with hydrazine hydrate(12.5 g, 0.25 M) in appropriate ethanol (30 mL) for 2 h. The progressof the reaction was monitored by TLC. After cooling the reactionmixture to room temperature, the mixtures were filtered to givewhite solid crude products without purification. Next, indolehydrazide(3, 1.0 mmol) in ethanol (30 mL) was added dropwiseinto the appropriate aldehyde (1.5 mmol-equiv.) and a few drops ofpropionic acid; the mixture was stirred and refluxed for 2.5 h. Aftercooling, the precipitates were filtered and washed several times bymethanol to yield the crystal substances 4aeu., 15317-58-5

As the paragraph descriping shows that 15317-58-5 is playing an increasingly important role.

Reference£º
Article; Ju, Zhiran; Su, Mingzhi; Hong, Jongki; La Kim, Eun; Moon, Hyung Ryong; Chung, Hae Young; Kim, Suhkmann; Jung, Jee H.; European Journal of Medicinal Chemistry; vol. 180; (2019); p. 86 – 98;,
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.50820-65-0,Methyl 1H-indole-6-carboxylate,as a common compound, the synthetic route is as follows.,50820-65-0

To a solution of methyl 1H-indole-6-carboxylate (17.5 g, 99.9 mmol, 1.0 eq) in i-PrOH (200 mL) was added cyclopent-2-en-1-one (16.4 g, 199.8 mmol, 16.7 mL, 2.0 eq) and SnCl2*2H2O (2.25 g, 9.99 mmol, 831.8 muL, 0.1 eq) under N2. After addition, the mixture was stirred at room temperature for 16 h. The reaction mixture was concentrated and diluted with DCM (250 mL). The organic layer was separated and washed with H2O (200 mL), brine (200 mL), dried over anhydrous Na2SO4, filtered, and concentrated under reduced pressure to give a residue. The residue was purified by column chromatography (SiO2) to give compound 03-4-1 (22.4 g, 79percent yield).1H NMR (CDCl3, 400 MHz): delta 8.38 (s, 1 H) 8.17 (s, 1 H) 7.84 (d, J=8.8 Hz, 1 H) 7.66 (d, J=8.8 Hz, 1 H) 7.19 (d, J=2.01 Hz, 1 H) 3.97 (s, 3 H) 3.74-3.77 (m, 1 H) 2.77-2.83 (m, 1 H) 2.58-2.59 (m, 1 H) 2.39-2.48 (m, 3 H) 2.15-2.17 (m, 1 H).

50820-65-0 Methyl 1H-indole-6-carboxylate 639844, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; KYRAS THERAPEUTICS, INC.; VACCA, Joseph P.; LI, Dansu; (587 pag.)WO2017/96045; (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.30448-16-9,7-Methyl-1H-indole-3-carboxylic acid,as a common compound, the synthetic route is as follows.

The bispyridine ester amine compound (200 mg, 0.99 mmol) in Example 1 and 7-methyl-1H-indole-3-carboxylic acid (170 mg, 0.99 mmol) were dissolved in DMF (5 ml), DCC (230 mg, 1.09 mmol) was added to the solution, and then the mixture was stirred at 80 C. for 8 hours. After the reaction was completed, the product was washed and filtered to yield a target compound as a white solid (30 ml, 7%) by chromatography (methanol:dichloromethane=1:30)., 30448-16-9

30448-16-9 7-Methyl-1H-indole-3-carboxylic acid 14810856, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY; US2009/258876; (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.1074-86-8,1H-Indole-4-carbaldehyde,as a common compound, the synthetic route is as follows.

General procedure: In a flame-dried Schlenk bottle under argon atmosphere, Grignard reagent B (10.2 mol) was added to the Schlenk bottle. Then, in an ice-water bath, a solution of 1H-indole-4-carbaldehyde A (10 mmol) in anhydrous THF (10 mL) was added to the Schlenk bottle. Subsequently, the reaction mixture was moved to an oil bath, which was refluxed at 70 o C overnight. After the completion of the reaction indicated by TLC, the reaction mixture was quenched by saturated ammonium chloride solution and was extracted by ethyl acetate for three times. The combined organic layer was dried by anhydrous sodium sulfate, which was concentrated under the reduced pressure. The resulted residue was purified through flash chromatography on silica gel to afford the pure 4-indolylmethanols 1.

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

Reference£º
Article; Liu, Jin-Xi; Zhu, Zi-Qi; Yu, Lei; Du, Bai-Xiang; Mei, Guang-Jian; Shi, Feng; Synthesis; vol. 50; 17; (2018); p. 3436 – 3444;,
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.51417-51-7,7-Bromoindole,as a common compound, the synthetic route is as follows.

51417-51-7, General procedure: To a 10 mL flame-dried Schlenk tube equipped with a stirring bar, indole1 (0.2 mmol), alpha-amido-sulfone 2 (0.2 mmol), and K2S2O8 (108.1mg, 0.4 mmol) were added. Toluene (1.2 mL) was injected into thetube at r.t. After stirring for 48 h, the mixture was purified by silica gelchromatography to afford the desired product 3.

As the paragraph descriping shows that 51417-51-7 is playing an increasingly important role.

Reference£º
Article; Wu, Xiaoyan; Xue, Lu; Luo, Shilong; Jia, Shiqi; Ao, Jun; Qin, Wenling; Synthesis; vol. 49; 22; (2017); p. 5017 – 5024;,
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.2338-71-8,5-Fluoro-1H-indole-3-carbaldehyde,as a common compound, the synthetic route is as follows.

Add III-6 (0.50g, 3.07mmol), DMAP (75mg, 0.61mmol), DIEA (1.52mL, 9.21mmol) to 100mL three-necked flask, stir and dissolve with 10mL acetonitrile, slowly add at 05C Benzene 4-trifluoromethylbenzenesulfonyl chloride (IV-7, 0.90 g, 3.68 mmol) in 10 mL of acetonitrile solution, after completion of the addition, stirring was continued for 2 h under low temperature conditions.TLC monitoring of raw material reactionsCompletely, concentrate the reaction solution, dissolve it with 20 mL of ethyl acetate, wash with 25 mL of water, and extract twice with ethyl acetate (15 mL¡Á2)The organic phase is washed with a saturated sodium chloride solution and dried over anhydrous sodium sulfate; suction filtered, and the filtrate is dried and then subjected to column chromatography ( petroleum ether:Ethyl acetate = 10:1 rinse),After drying, 0.91 g of khaki solid V-15 was obtained.The yield was 80.25%., 2338-71-8

As the paragraph descriping shows that 2338-71-8 is playing an increasingly important role.

Reference£º
Patent; China Pharmaceutical University; Xu Yungen; He Guangchao; Huang Qungang; Liang Tingting; Zhang Shan; Zhu Qihua; (35 pag.)CN109942545; (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.387-43-9,4-Fluoroindole,as a common compound, the synthetic route is as follows.

To a solution DMF (0.670 ml8.653 mmol) in dichloromethane (2.5 mL) cooled to -15 ¡ãC was added dropwise phosphorus oxychloride (0.400 mL; 4.291 mmol). After 15 min at -15 ¡ãC, a solution of 4-fluoro-1 /-/-indole (0.500 g; 3.700 mmol) in dichloromethane (2 mL) was added. The reaction mixture was allowed to warm to room temperature and was stirred at room temperature overnight. A saturated sodium bicarbonate solution was added and the reaction mixture was extracted with dichloromethane. The organic phase was dried over magnesium sulfate, filtered and concentrated under reduced pressure. Purification by flash chromatography on silica gel using ethyl acetate (50percent) in heptane as eluent furnished 0.144 g (24percent) of 4-fluoro- 1 H-indole-3-carbaldehyde as a beige solid. ESI/APCI(+): 164. ESI/APCI(-): 162 (M-H).

387-43-9, As the paragraph descriping shows that 387-43-9 is playing an increasingly important role.

Reference£º
Patent; KATHOLIEKE UNIVERSITEIT LEUVEN; BARDIOT, Dorothee; CARLENS, Gunter; DALLMEIER, Kai; KAPTEIN, Suzanne; McNAUGHTON, Michael; MARCHAND, Arnaud; NEYTS, Johan; SMETS, Wim; WO2013/45516; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4771-48-6,4-Methyl-1H-indole-3-carbaldehyde,as a common compound, the synthetic route is as follows.

The intermediate 1- (3,4,5-trimethoxyphenyl) propan-1-one (448 mg, 2 mmol) was dissolved in a solution of piperidine (0.1 mL) in toluene (6 mL), and 4-methyl-1H-indole-3-carboxaldehyde (156.8mg, 0.8mmol), reacted at 130 C for 4h,The organic phase was spin-dried, and the remaining crude product was recrystallized from ethanol to obtain the target compound (E)-2-methyl-3-(4-methyl-1H-indol-3-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (1) 230mg,The yield was 51.3%.

4771-48-6, 4771-48-6 4-Methyl-1H-indole-3-carbaldehyde 2762437, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Ningxia Medical University; Zhuang Chunlin; Shi Ying; Cong Hui; Zhang Wannian; Huang Jiaxuan; Yu Jianqiang; Xu Lijuan; Qu Zhuo; (21 pag.)CN110526854; (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.387-43-9,4-Fluoroindole,as a common compound, the synthetic route is as follows.

Take 135 mg (1 mmol) of 4-fluoroindole, 132.6 mg (1.3 mmol) of 5-hydroxy-2-pentanone and 20.48 mg (0.04 mmol) of tris(pentafluorophenyl)boron in a 10 mL reaction tube. The reaction was stirred at 40 C, and monitored by TLC until hydrazine disappeared, extracted with 3¡Á20 mL ethyl acetate, and the organic phase was washed with saturated brine.The organic layer was dried over anhydrous sodium sulfate, and the solvent ethyl acetate was evaporated to dryness (methanol ethyl ether: 20:1) to afford 3-(tetrahydro-2-methyl-2-furanyl)-4-fluoro-1H-indole product 175 mg, yield: 80%.

387-43-9, As the paragraph descriping shows that 387-43-9 is playing an increasingly important role.

Reference£º
Patent; Huazhong University of Science and Technology; Wang Shijun; Xia Sang; Tang Xiangying; (18 pag.)CN109912579; (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

2338-71-8, 5-Fluoro-1H-indole-3-carbaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The intermediate 1- (3,4,5-trimethoxyphenyl) propan-1-one (336 mg, 1.5 mmol)With 5-fluoro-1H-indole-3-carboxaldehyde (81.6mg, 0.5mmol) in ethanol (5mL) solution,Add piperidine (0.3mL) and stir at 95 C for 48h.The organic phase was spin-dried, and the remaining crude product was recrystallized from ethanol to obtain the target compound.(E) -3- (5-fluoro-1H-indol-3-yl) -2-methyl-1- (3,4,5-trimethoxyphenyl) prop-2-en-1-one94.1mg, yield 51%, 2338-71-8

As the paragraph descriping shows that 2338-71-8 is playing an increasingly important role.

Reference£º
Patent; Ningxia Medical University; Zhuang Chunlin; Shi Ying; Cong Hui; Zhang Wannian; Huang Jiaxuan; Yu Jianqiang; Xu Lijuan; Qu Zhuo; (21 pag.)CN110526854; (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