Category: 399-52-0

Fang, Songjia’s team published research in Chemical Communications (Cambridge, United Kingdom) in 2019 | CAS: 399-52-0

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Depending on which substituents are present, fluoroaromatic intermediates can be converted into fluorinated or fluorine-free commercial end products.Fluorine-containing aromatics have been incorporated into drugs (hypnotics, tranquilizers, antiinflammatory agents, analgesics, antibacterials).Safety of 5-Fluoro-1H-indole

The author of 《Palladium-catalyzed regioselective C-H alkynylation of indoles with haloalkynes: access to functionalized 7-alkynylindoles》 were Fang, Songjia; Jiang, Guangbin; Li, Meng; Liu, Zhenying; Jiang, Huanfeng; Wu, Wanqing. And the article was published in Chemical Communications (Cambridge, United Kingdom) in 2019. Safety of 5-Fluoro-1H-indole The author mentioned the following in the article:

A Pd-catalyzed uniquely regioselective C-H alkynylation of indoles was described. In this protocol, simple and readily available haloalkynes are employed as efficient alkynylating reagents, affording functionalized 7-alkynylindoles in moderate to good yields. Also, further transformations of 7-alkynylated products were performed, which demonstrated the potential application of this method in organic synthesis. The results came from multiple reactions, including the reaction of 5-Fluoro-1H-indole(cas: 399-52-0Safety of 5-Fluoro-1H-indole)

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Depending on which substituents are present, fluoroaromatic intermediates can be converted into fluorinated or fluorine-free commercial end products.Fluorine-containing aromatics have been incorporated into drugs (hypnotics, tranquilizers, antiinflammatory agents, analgesics, antibacterials).Safety of 5-Fluoro-1H-indole

Referemce:
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

Chang, Chieh-Yu’s team published research in Chemical Communications (Cambridge, United Kingdom) in 2019 | CAS: 399-52-0

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Fluorine-containing aromatics have been incorporated into crop-protection chemicals (herbicides, insecticides, fungicides). Liquid crystals, positron emission tomography, and imaging systems represent new areas where fluoroaromatics and fluoroheterocyclics have gained attention.SDS of cas: 399-52-0

In 2019,Chemical Communications (Cambridge, United Kingdom) included an article by Chang, Chieh-Yu; Lin, Yu-Huan; Wu, Yen-Ku. SDS of cas: 399-52-0. The article was titled 《Palladium-catalyzed N1-selective allylation of indoles with allylic alcohols promoted by titanium tetraisopropoxide》. The information in the text is summarized as follows:

The direct N1-selective allylation of indoles with allylic alcs. has been accomplished by synergistic functions of palladium catalysts and titanium tetraisopropoxide. The site selectivity is notably different from that observed in other related transition metal-catalyzed approaches. This chem. provides a facile route to a variety of allylated indoles I (R = 5-MeO, 4-MeO, 6-MeO, etc.; R1 = Me, H, Ph, etc.) in synthetically useful yields. The utility of this simple allylation reaction was demonstrated with the first total synthesis of (+)-N-(4′-hydroxyprenyl)-cyclo(alanyltryptophyl), which was completed in five steps, starting from L-tryptophan Me ester hydrochloride. The experimental part of the paper was very detailed, including the reaction process of 5-Fluoro-1H-indole(cas: 399-52-0SDS of cas: 399-52-0)

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Fluorine-containing aromatics have been incorporated into crop-protection chemicals (herbicides, insecticides, fungicides). Liquid crystals, positron emission tomography, and imaging systems represent new areas where fluoroaromatics and fluoroheterocyclics have gained attention.SDS of cas: 399-52-0

Referemce:
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

Downstream synthetic route of 399-52-0

The synthetic route of 399-52-0 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.399-52-0,5-Fluoro-1H-indole,as a common compound, the synthetic route is as follows.,399-52-0

General procedure: A method for synthesizing compound III-1 wherein R1, R2 and R3 are simultaneously hydrogen in the formula III, the method comprising the steps of:(1) Add to a 50 mL round bottom flask1.0mmol indole(In the formula I, R1, R2, and R3 are both hydrogen) and1.0 mmol (0.140 g) of hexamethylenetetramine, then 2 mL of N,N-dimethylformamide (DMF), stirred in a magnetic stirrer to dissolve the solid, followed by the addition of 0.05 mmol (0.012 g) of crystalline trichloride Aluminum, connected to a reflux condenser, heated at 120 C, the reaction progress was monitored by TLC, and the reaction was cooled to room temperature after 1 h to prepare a suspension;(2) The suspension prepared in the step (1) is suction filtered with a funnel padded with diatomaceous earth.The filter cake was washed well with ethyl acetate, suction filtered, and the above operation was repeated until the filtrate had no product, and all the filtrates were combined.Dilute with 15 mL of saturated saline solution, disperse and separate the layers, and the aqueous layer was further extracted with ethyl acetate three times.Each time 10 mL, the ethyl acetate layer was combined and washed with 10 mL of 2 mol/L diluted hydrochloric acid.Wash with 10 mL of saturated sodium bicarbonate solution, and finally wash with 10 mL of saturated brine.The washed ethyl acetate layer was dried over anhydrous sodium sulfate, and after drying, the desiccant was filtered off.Then use a rotary evaporator to recover the solvent to concentrate the product, and finally,The residue is subjected to silica gel column chromatography using a mixture of n-hexane-ethyl acetate (V/V = 2:1) as an eluent to obtain a purified product.The mass of the compound III-indole-3-carbaldehyde is 0.137g,The product yield was 94%.

The synthetic route of 399-52-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Yancheng Jin Ming Pharmaceutical Co., Ltd.; Yancheng Normal College; Wang Qingdong; Yang Zijian; Fang Yue; Wu Zhen; Zeng Bubing; Yang Jinming; Hu Chaojun; Zhao Yujun; (19 pag.)CN108329249; (2018); 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