Day: September 11, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4769-96-4,6-Nitro-1H-indole,as a common compound, the synthetic route is as follows.,4769-96-4

AddiV-bromosuccinamide (NBS) to 6-nitroindole 1 (22.72 g, 140.12 mmol) dissolved in tetrahydrofuran (600 mL) and allow the resulting mixture to stir for 18 hours. Quench the reaction mixture with saturated aqueous sodium thiosulfate solution (600 mL), dilute with ethyl acetate (EtOAc) (600 mL), and separate the layers. Sequentially, wash the organic layer with saturated aqueous sodium bisulfate (100 mL), saturated aqueous sodium bicarbonate (100 mL), water (100 mL), and brine (100 mL). Dry the resulting organic layer over Na2SO4 and filter. Concentrate the filtrate to give a yellow solid. Recrystallize the solid from dichloromethane and hexane to give 29.21 g of the title compound (86 %). LRMS (API ES+) = 263.0 (M+Na).

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

Reference£º
Patent; ELI LILLY AND COMPANY; WO2007/87488; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.90271-86-6,5-Bromo-3-cyanoindole,as a common compound, the synthetic route is as follows.

90271-86-6, General procedure: A solution of the appropriate 1H-indole-3-carbonitriles 5a-c or1-methylindole-3-carbonitriles 6a-c (5 mmol) and thiosemicarbazide(5 mmol) in trifluoroacetic acid (5 ml) was heated at60 C for 3.5 h. The reaction mixture was then poured into ice andslowly neutralized with NaHCO3 saturated solution. The obtainedprecipitate was filtered off, washed with water, cyclohexane anddiethyl ether

90271-86-6 5-Bromo-3-cyanoindole 3623354, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Cascioferro, Stella; Parrino, Barbara; Petri, Giovanna Li; Cusimano, Maria Grazia; Schillaci, Domenico; Di Sarno, Veronica; Musella, Simona; Giovannetti, Elisa; Cirrincione, Girolamo; Diana, Patrizia; European Journal of Medicinal Chemistry; vol. 167; (2019); p. 200 – 210;,
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.1111638-02-8,5-Bromo-2-methyl-7-azaindole,as a common compound, the synthetic route is as follows.

5.1.1.4 5-Bromo-3-(1-(2,6-dichloro-3-fluorophenyl)ethyl)-2-methyl-1H-pyrrolo[2,3-b]pyridine (22) To a solution of compound 20 (450 mg, 2.13 mmol) in DCM (10 mL) Trifluoromethanesulfonic acid (TfOH, 1.28 g, 8.53 mmol) and 1-(2,6-Dichloro-3-fluorophenyl)ethanol (1.63 g, 8.53 mmol) was added dropwise. After stirring at 25 C under N2 for 16 h, the mixture was quenched with sat. Sodium bicarbonate (NaHCO3) solution, extracted with DCM (100 mL * 3). The organic phase was washed with water (20 mL * 2), brine (20 mL * 2), dried over Na2SO4. After filtering, the organic phase was concentrated and purified by column chromatography on silica (DCM:MeOH = 200:1) to give 22 as a white solid (650 mg, 75.8% yield). 1H NMR (400 MHz, DMSO-d6) delta 11.66 (s, 1H, NH), 8.12 (s, 1H, Ar-H), 7.87 (s, 1H, Ar-H), 7.54-7.50 (dd, J = 8.9, 5.1 Hz, 1H, Ar-H), 7.39-7.34 (t, J = 8.7 Hz, 1H, Ar-H), 5.15-5.12 (q, J = 7.4 Hz, 1H, CH), 2.18 (s, 3H, CH3), 1.86-1.83 (d, J = 7.5 Hz, 3H, CH3).

1111638-02-8, The synthetic route of 1111638-02-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Liu, Na; Wang, Yanfen; Huang, Gongchao; Ji, Conghui; Fan, Wei; Li, Haitao; Cheng, Ying; Tian, Hongqi; Bioorganic Chemistry; vol. 65; (2016); p. 146 – 158;,
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

245-08-9, 5H-Pyrido[3,2-b]indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

One 100 mLThe flask Intermediate (4) (0.5 g, 1.005 mmol), delta-carboline(d-carboline)0.2 g (1.105mmol), CuI 24 mg (0.126 mmol), 1,10 phenanthroline (1,10 phenanthroline) 45mg (0.251 mmol), cesium carbonate (cesium carbonate, Cs2CO3) 0.7 g (2.010 mmol) and dimethylformamide (dimethylformamide, DMF) (40 mL) and mixed, and then,stirred for 12 hours at 120 ~ 130C. The reaction was cooled to room temperature and then terminated and purified by silica gel column chromatography to give compound (4-33) 0.2 g (Yield: 40%) of a white solid was obtained., 245-08-9

As the paragraph descriping shows that 245-08-9 is playing an increasingly important role.

Reference£º
Patent; WS Co.,Ltd; Ko, Byung Soo; Oh, Yu Jin; (61 pag.)KR2016/50891; (2016); 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

29906-67-0, 1-Methyl-5-nitro-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Silver (I) oxide (1 eq.) was added to a stirred solution of indole (1eq.) and benzyl bromide (1 eq.) in dioxane (1 mL/mmol of indole) ina microwave tube under nitrogen gas. The reaction was sealed andstirred at 60 C for 20 h. EtOAc (2 mL/mmol of indole) was added tothe reaction. The reaction was then filtered through celite and thefiltrate was rotovapped. Product was purified by column chromatographyto give a yellow solid; 25-45%; 1H NMR (DMSO): delta 8.42 (d,J 2.3 Hz, 1H), 8.02 (dd, J 9.1, 2.3 Hz, 1H), 7.93e7.84 (m, 2H), 7.60(d, J 9.1 Hz, 1H), 7.44 (d, J 8.3 Hz, 3H), 4.21 (s, 2H), 3.83 (d,J 4.1 Hz, 6H); 13C NMR (DMSO): delta166.59, 147.18, 140.80, 140.05,132.12, 129.82, 129.25, 127.93, 126.82, 116.99, 116.29, 116.03, 110.86,52.45, 33.30, 30.65

29906-67-0, As the paragraph descriping shows that 29906-67-0 is playing an increasingly important role.

Reference£º
Article; Martinez, Anastasia A.; Espinosa, Bianca A.; Adamek, Rebecca N.; Thomas, Brent A.; Chau, Jennifer; Gonzalez, Edwardo; Keppetipola, Niroshika; Salzameda, Nicholas T.; European Journal of Medicinal Chemistry; vol. 157; (2018); p. 1202 – 1213;,
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.103858-53-3,Ethyl 6-bromoindole-2-carboxylate,as a common compound, the synthetic route is as follows.

General procedure: To ethyl 1H-indole-2-carboxylate (1.3 g, 6.89 mmol) in THF at 0 .was added lithium aluminumhydride solution (1M, in THF 0.29 g, 1.54 mmol) dropwise and the reaction mixture was stirred for 3.5 hours at0 . The reaction mixture was quenched with H2O, 15% NaOH, and H2O before it was filtered and rinsed withTHF. Reaction mixture was dried (anhydrous Na2SO4) and evaporation of the solvent gave 1.1 g (96% yield) of thecrude (1H-indol-2-yl)methanol which was used directly in the next step.

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

Reference£º
Article; Jiang, Zeng-Qiang; Miao, Da-Zhuang; Tong, Yao; Pan, Qiang; Li, Xiao-Tong; Hu, Ren-He; Han, Shi-Qing; Synthesis; vol. 47; 13; (2015); p. 1913 – 1921;,
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.1092114-59-4,3-Iodo-1H-indole-5-carbonitrile,as a common compound, the synthetic route is as follows.

Preparation of compound 69b: 3-iodo-l-tosyl-l/7-indole-5-carbonitrileTo a solution of 3-iodo-l//-indole-5-carbonitrile (2 g, 7.40 mmol) in DMF (20 mL) was added 60% NaH (538 mg, 22.38 mmol) portion wise at 0 C and the reaction was stirred for 10 min RT. To the above mixture at 0 C, p-TsCl (2.2 g, 11.19 mmol) solution in DMF (4 mL) was added and stirred for further 2 h at RT. The reaction was quenched with ice cold H20 (20 mL). The resulting suspension was filtered and the solid was washed with H20 (10 mL) and dried. The crude was purified with silica gel chromatography (eluent: 20% EtOAc in petroleum ether) to afford 3-iodo-l-tosyl-l//-indole-5-carbonitrile (3.0 g, 95.5%) as an off brown solid. .H NMR (400MHz, DMSO-d6): delta 8.30 (s, 1H), 8.13 (d, J=8.8Hz, 1H), 7.98 (d, J=8.4Hz, 2H), 7.87-7.81 (m, 2H), 7.43 (d, J=8.0Hz, 2H), 2.32 (s, 3H)., 1092114-59-4

As the paragraph descriping shows that 1092114-59-4 is playing an increasingly important role.

Reference£º
Patent; AMGEN INC.; WANG, Hui-Ling; CEE, Victor, C.; HERBERICH, Bradley, J.; JACKSON, Claire, L., M.; LANMAN, Brian, Alan; NIXEY, Thomas; PETTUS, Liping, H.; REED, Anthony, B.; WU, Bin; WURZ, Ryan; TASKER, Andrew; WO2012/129338; (2012); 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

166104-19-4, tert-Butyl 5-nitro-1H-indole-1-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 2; Following the procedure set forth in Example 1 (A) above, indole derivatives were deprotected using TFE or HFIP in a microwave reactor at 150 C. as set forth in Table 1 below., 166104-19-4

As the paragraph descriping shows that 166104-19-4 is playing an increasingly important role.

Reference£º
Patent; Roch Palo Alto LLC; US2009/203910; (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

6146-52-7,6146-52-7, 5-Nitroindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Nitro-lH-indole (325 mg, 2.0 mmol)In dichloromethane (6 mL) was added di-tert-butyl dicarbonateEster (524 mg, 2.4 mmol),Stirred at 0 C for 5 minutes,A further catalytic amount of 4-dimethylaminopyridine (3 mg, 0.025 mmol) was added,Stirring is then continued for 30 minutes at room temperature.Quenched by adding water (2 mL)Extract with dichloromethane (15 mL x 3).The combined organic phase was washed with water (20 mL)Saturated brine (15 mL ¡Á 2)Dried over anhydrous sodium sulfate,The solvent was distilled off under reduced pressure,Obtained as a gray solid (526 mg, 100%),Directly used for the next reaction.

As the paragraph descriping shows that 6146-52-7 is playing an increasingly important role.

Reference£º
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Wen Liang; Zheng Jinfu; Zhang Jin; Wu Shoutao; Yuan Xiaofeng; Lin Runfeng; Wang Xiaojun; Zuo Yinglin; Zhang Yingjun; (21 pag.)CN104311541; (2017); B;,
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

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) 6-Aminoindole was prepared from 6-nitroindole in a manner similar to that described in Example 5b.

4769-96-4, 4769-96-4 6-Nitro-1H-indole 78502, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Hoffmann-La Roche Inc.; US6228877; (2001); 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