Day: September 15, 2020

4769-96-4,4769-96-4, 6-Nitro-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(a) Step 1 6-Nitroindole (1.0 g, 6.2 mmol) was successively added with acetic acid (2.5 mL), water (5.0 mL), and hexamethylenetetramine (1.2 g, 8.4 mmol), and then the mixture was stirred overnight at 120C in a sealed tube. The reaction mixture was added with water, and the precipitated solid was collected by filtration, and then dried to obtain 6-nitro-1H-indole-3-carboxaldehyde (0.91 g, 77%). 1H NMR (300 MHz, DMSO-d6) delta 8.12 (d, J = 8.8 Hz, 1H), 8.27 (d, J = 8.8 Hz, 1H), 8.44 (s, 1H), 8.66 (s, 1H), 10.02 (s, 1H).

The synthetic route of 4769-96-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; The University of Tokyo; Riken; NAGANO Tetsuo; OKABE Takayoshi; KOJIMA Hirotatsu; SAITO Nae; NAKANO Hirofumi; ABE Masanao; TANAKA Akiko; HONMA Teruki; YOKOYAMA Shigeyuki; TSUGANEZAWA Keiko; YUKI Hitomi; EP2565192; (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.15861-24-2,Indole-5-carbonitrile,as a common compound, the synthetic route is as follows.

Compound 14 (15 g) was taken in methanol (300 ml) and water (30 ml) mixture and NaOH (4.6 g) and Kl (20.89 g) were added. Iodine (30.51 g) was added portion wise at RT. Reaction mixture was stirred at RT for 6 hr. Reaction was monitored using LCMS & TLC. Reaction mixture was diluted with water (1000 ml) and the precipitated solid was filtered-off and dried under vac- uum. Yellow solid obtained was dissolved in DCM and dried over sodium sulphate and concentrated under vacuum. 25 g of pure solid compound 15 was obtained. (0552) 1 H NMR 300 MHz, DMSO-d6: delta 12.09 (s, 1 H), 7.82 – 7.73 (m, 2H), 7.64 – 7.47 (m, 2H).

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

Reference£º
Patent; BASF SE; RHEINHEIMER, Joachim; RATH, Rakesh; KULKARNI, Sarang; ROSENBAUM, Claudia; WIEBE, Christine; BRAHM, Lutz; SIEPE, Isabella; HADEN, Egon; ROEHL, Franz; KHANNA, Smriti; SCHIFFER, Helmut; KREMZOW-GRAW, Doris; POONOTH, Manojkumar; (285 pag.)WO2019/57660; (2019); 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

26340-49-8, 2-Iodo-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To the solution of iodoindole 6 (200 mg, 0.82 mmol) in DMF (2.8 mL) at 0 C was added powderedKOH (70 mg, 1.24 mmol). The heterogeneous mixture was stirred at 0 C for 5 min and treated withBnBr (154 mg, 0.90 mmol). After stirring at 0 C for 10 min, the reaction mixture was diluted with Et2O(15 mL) and quenched with brain (10 mL). The layers were separated and the aqueous layer was6extracted with Et2O (1 x 15 mL). The organic layers were combined, dried over Na2SO4, andconcentrated in vacuo. The residue was purified by flash chromatography (silica gel, hexane/AcOEt =50:1) to afford 2d (267 mg, 97% yield) as a white solid., 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

166104-20-7, 1-Boc-5-Aminoindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 2-chioro-3-nitro-6-(trifluoromethyl)pyridine (1.0 g, 4.4 rnmoi)and tert-hulyl 5-amino-1H-indoie-1-carboxylate (0.59 g, 4.4 mmol) in DMF (20 mL) was heated at 100 ¡ãC for 3 h. 4-Fluorobenzaldehyde (0.60 g. 4.9 mmol) was added to the mixture and the reaction was stirred for 30 mm followed by addition of sodium dithionite (2.3g. 13.2 rnrnol). After 12 h at100 ¡ãC the reaction was cooled, diluted with EtOAc (100 mnL), and washed with F120 (50 mL x 3). The organic layer was dried (Na2504), and concentrated in vacuo. Purification (FCC. 5i02, EtOAc/hexanes) afforded the title compound (1.1 g, 50percent). MS ESI): mass caicd. for C76H20F4N407, 496.1; mn/z found, 497.0 [M?++{it., 166104-20-7

As the paragraph descriping shows that 166104-20-7 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; BERRY, Cynthia G.B.; CHEN, Gang; JOURDAN, Fabrice Loic; LEBOLD, Terry Patrick; LIN, David Wei; PENA PINON, Miguel Angel; RAVULA, Suchitra; SAVALL, Bradley M.; SWANSON, Devin M.; WU, Dongpei; ZHANG, Wei; AMERIKS, Michael K.; (407 pag.)WO2016/176460; (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.16096-32-5,4-Methyl-1H-indole,as a common compound, the synthetic route is as follows.

General procedure: A mixture of xanthen-9-ol 1 (0.040 g, 0.2 mmol) and 2a (0.024 g, 0.2 mmol) was stirred in a tube at room temperature in BmimBF4 (0.5 mL) until the disappearance of the starting 2a (24 h, checked by thin-layer chromatography, TLC). After completing, the reaction mixture was extracted by ethyl ether (3¡Á15 mL), then concentrated and isolated by flash chromatograph to afford the pure product 3a (0.054 g, yield: 92%).

16096-32-5, 16096-32-5 4-Methyl-1H-indole 85282, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Liu, Ling-Yan; Wang, Bing; Yang, Hong-Mei; Chang, Wei-Xing; Li, Jing; Tetrahedron Letters; vol. 52; 43; (2011); p. 5636 – 5639;,
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.252978-89-5,tert-Butyl 4-(1H-indol-4-yl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

EXAMPLE 13 1-[(2,5-Dichloro-3-thienyl)sulfonyl]-4-(1-piperazinyl)-1H-indole Hydrochloride (Scheme 1) The title compound was prepared from 4-(4-boc-piperazinyl)-indole and 2,5-dichloro-3-thienylsulfonyl chloride according to Method 3: 1H NMR (270 MHz, DMSO-d6) delta 9.24 (br, 1H), 7.78 (d, J=5 Hz, 1H), 7.72 (s, 1H), 7.57 (d, J=8 Hz, 1H), 7.29 (t, J=8 Hz, 1H), 7.01 (d, J=5 Hz, 1H), 6.86 (d, J=8 Hz, 1H), 3.31 (m, 8H). MS (ESI+) for m/z 416 (M+H)+., 252978-89-5

Big data shows that 252978-89-5 is playing an increasingly important role.

Reference£º
Patent; Caldirola, Patrizia; Nilsson, Bjorn M.; Johansson, Gary; US2002/165251; (2002); 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

1000340-39-5, 3-Bromo-4-chloro-7-azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,1000340-39-5

Step 2: A solution of C38 (8 g, 34.632 mM) in THF (160 mL) was cooled to -780C, treated with n-BuLi (1.6M, 5OmL, 79.63 mM), and stirred for 30 min. at -780C. The cold solution was then slowly treated with DMF (5.056 g, 69.264m M). The reaction mixture was allowed to warm to 25C, stirred for 2 hr., and treated with water (2 mL) to quench the reaction. The reaction mixture was concentrated under reduced pressure and treated with saturated aq. NH4CI (28 mL), and the solids were collected and dried under reduced pressure. The resultant pale yellow solid (3.5g, 52%) was then purified using silica gel column to provide 4-chloro-1 H-pyrrolo[2,3-b]pyridine-3-carbaldehyde (C39). 1HNMR(CDCI3) 8: 12.6-12.8 (b,1 H),10.4-10.6 (s,1 H),8.26-8.3 (d,1 H),8.12-8.18 (s,1 H),7.26-7.3 (d,1 H). Mass:(M+1 ) 181 calculated for mol. form. C8H5CIN2O.

1000340-39-5 3-Bromo-4-chloro-7-azaindole 24729570, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; PFIZER PRODUCTS INC.; WO2008/12635; (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

16136-52-0, 4-Cyanoindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The calcium or magnesium salt (0.025 mmol, 10 mol%) and Michael acceptor (0.25 mmol) were dissolved in solvent (0.5 mL), and the mixture was stirred at r.t. for 30 min in a glass vial. The aromatic compound (0.5 mmol) was added and the reaction was stirred at the temperature indicated in Tables 2-9; reaction progress was monitored by TLC. When the reaction was complete, the solvent was evaporated under reduced pressure. The crude residue was purified by column chromatography to afford the product.

16136-52-0, 16136-52-0 4-Cyanoindole 3817602, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Feofanov, Mikhail N.; Anokhin, Maxim V.; Averin, Alexei D.; Beletskaya, Irina P.; Synthesis; vol. 49; 22; (2017); p. 5045 – 5058;,
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.

The title compound of this step is prepared by the method described in the third step of Example 1,4-methyl-2-(2-(piperazin-1-yl)pyrimidin-5-yl)oxazole-5-carboxamide dihydrochloride (500 mg, 1.38 mmol),3-(4-Chlorobutyl)-1H-indole-5-carbonitrile (386 mg, 1.66 mmol), anhydrous sodium carbonate (878 mg, 8.28 mmol)Sodium iodide (63 mg, 0.42 mmol) was prepared in acetonitrile (15 mL) at 90 C for 36 hours.The obtained crude product was further purified by silica gel chromatography (dichloromethane:methanol (V:V)=30:1) to give the title compound(light yellow solid, 492 mg, 73.6%)., 143612-79-7

143612-79-7 3-(4-Chlorobutyl)-1H-indole-5-carbonitrile 9881123, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Jin Chuanfei; Zhong Wenhe; Liang Haiping; Zhang Yingjun; (57 pag.)CN109574993; (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.4771-50-0,7-Methylindole-3-carboxyaldehyde,as a common compound, the synthetic route is as follows.

General procedure: An equimolar mixture of Gewald adducts (5CN, 6CN, 7CN and 8CN) and substituted indole-carboxaldehydes in absolute ethanol with 0.5 mL of acetic acid was stirred under room temperature for 24 hs. Water was addedand the solid that precipitated out was filtered under vacuum, washed with water, dried and recrystallized from absolute ethanol (Scheme 1) according previously methodology [20].

4771-50-0, 4771-50-0 7-Methylindole-3-carboxyaldehyde 260389, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Felix, Mayara B.; de Souza, Edson R.; de Lima, Maria do C.A.; Frade, Daiana Karla G.; Serafim, Vanessa de L.; Rodrigues, Klinger Antonio da F.; Neris, Patricia Lima do N.; Ribeiro, Frederico F.; Scotti, Luciana; Scotti, Marcus T.; de Aquino, Thiago M.; Mendonca Junior, Francisco Jaime B.; de Oliveira, Marcia R.; Bioorganic and Medicinal Chemistry; vol. 24; 18; (2016); p. 3972 – 3977;,
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