Day: October 14, 2020

868656-97-7, Methyl 6-bromo-1H-indole-3-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

868656-97-7, Intermediate Preparation 41; 6-Bromo-l -methyl- IH- indole-3-carboxylic acid methyl ester; To a mixture of 6-bromo- leta-indole-3-carboxylic acid methyl ester (100 mg, 0.394 mmol), potassium carbonate (163 mg, 1.18 mmol) in DMF is added iodomethane (30 muL, 0.47 mmol). The reaction mixture is stirred for 1.5 h. Additional iodomethane (10 muL) is added and the reaction is stirred for 30 minutes. The reaction mixture is diluted with dichloromethane and filtered. The filtrate is concentrated under high vacuum, diluted with ethyl acetate, and concentrated to give the title compound (105 mg, 99%). ES/MS m/e 270.0 (M + 2).

868656-97-7 Methyl 6-bromo-1H-indole-3-carboxylate 11499811, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; ELI LILLY AND COMPANY; WO2009/12125; (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.1670-83-3,Indole-7-carboxylic acid,as a common compound, the synthetic route is as follows.

Example 75; Preparation of [rac]-1H-Indole-7-carboxylic acid (4-tert-butyl-benzyl)-[2-(4-chloro-phenyl)-propyl]-amide 79; To a solution of 81 mg of 1H-indole-7-carboxylic acid (0.5 mmol) and 161 mg of TBTU (0.5 mmol) in 2 ml DMF, were added 0.43 ml (2.5 mmol) of N,N-diisopropylethyl amine. After stirring for 5 min at rt, 158 mg (0.5 mmol) [rac]-(4-tert-butyl-benzyl)-[2-(4-chloro-phenyl)-propyl]-amine in 3.5 ml DMF was added. After stirring for 22 h at rt, the reaction mixture was diluted with 50 ml water and extracted twice with 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 (40 g silica gel; heptane/EtOAc 2:1) to give 203 mg (86%) of a off-white solid. MS(ISP) 459.4 (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

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.

Synthesis of 4-fluoro-1H-indole-3-carbaldehyde (Intermediate-23) To a 25 mL RB flask fitted with magnetic stirrer were added DMF (0.413 g) and POCl3 (0.623 g, 4 mmol) at 0¡ã C. under N2 atmosphere and the resulting mixture was stirred for 30 minutes at same temperature. Then Starting Material-4 (500 mg, 3.7 mmol) in DMF was added to the mixture and stirred at 40¡ã C. for 1 hour. After completion of the reaction the reaction mixture was cooled to 0¡ã C., quenched with NaOH solution and was extracted with ethyl acetate. Organic layers were concentrated to give crude material, which was then purified by silica-gel column chromatography eluting with hexane:EtOAc to give Intermediate-23 (230 mg) as brown material. LC-MS (M+H)+=164.2.

387-43-9, The synthetic route of 387-43-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Rao, Jagannath Madanahalli Ranganath; Venkatesham, Uppala; Doppalapudi, Sivanageswara Rao; Kenchegowda, Bommegowda Yadaganahalli; Fernand, George; George, Jenson; Madhavan, G R; Naidu, Gorle Paidapu; Kadambari, V. S. Naga Rajesh; Jagannath, S; Manivannan, R; Kumar, T Senthil; Kumar, B Siva Senthil; Mallikarjuna, Rayi; US2015/141650; (2015); 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.1011-65-0,Methyl 1H-indole-5-carboxylate,as a common compound, the synthetic route is as follows.,1011-65-0

Production Example 7 A 1.28 ml portion of phosphoryl chloride was added dropwise to 8 ml ofN,N-dimethylformamide under ice-cooling, followed by stirring at room temperature for 15 minutes. An 8 ml portion of an N,N-dimethylformamide solution of 2.00 g of methyl 1H-indole-5-carboxylate was added dropwise to this solution under ice-cooling, followed by stirring at room temperature for 1.5 hours. Under ice-cooling, 50 ml of water was added thereto and potassium carbonate was further added until the pH became 12, and the resulting solid was collected by filtration, washed with water and then dried over heating under a reduced pressure to obtain 2.19 g of methyl 3-formyl-1H-indole-5-carboxylate as a pale light brown solid.

The synthetic route of 1011-65-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Astellas Pharma Inc.; EP1988076; (2008); 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.875-30-9,1,3-Dimethyl-1H-indole,as a common compound, the synthetic route is as follows.

General procedure: To a solution of N-methylindoles (1.0mmol), sodium aryl sulfonates (0.5mmol), catalyst I2 (0.75mmol) and tert-Butyl hydroperoxide (1.5mmol) in methanol (2mL) were added. The reaction mixture was stirred at 80C for 12h. Then the reaction mixture was cooled to room temperature, diluted with brine (15mL) and extracted with EtOAc (3¡Á25mL). The organic layer dried over anhydrous MgSO4 and concentrated in vacuo. The residue was further purified by column chromatography on silica gel (Petroleum ether/EtOAc=5:1) to afford the compounds 6a, 7a-b, 8a-h, 9a-k, 10a-d with yield of 9%-95%.

875-30-9, The synthetic route of 875-30-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Xia, Qinqin; Bao, Xiaodong; Sun, Chuchu; Wu, Di; Rong, Xiaona; Liu, Zhiguo; Gu, Yugui; Zhou, Jianmin; Liang, Guang; European Journal of Medicinal Chemistry; vol. 160; (2018); p. 120 – 132;,
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.310886-79-4,Methyl 5-fluoro-1H-indole-3-carboxylate,as a common compound, the synthetic route is as follows.

A solution of thallium tris(trifmoroacetate) (8.45 g, 15.6 mmol) in TFA (35 mL) was added to a solution of 5-fluoro-li7-indole-3-carboxylic acid methyl ester (2 g, 10.4 mmol) in TFA (10 mL) at room temperature and stirred for 2 h. The reaction mixture was evaporated in vacuo and the resulting residue suspended in water (25 mL) before being treated with a solution of potassium iodide (5.2 g, 31.3 mmol) in water (50 mL). The reaction mixture was treated with dichloromethane (100 mL) and methanol (5 mL) and the resulting precipitate removed by filtration through celite.The organic layer was separated, washed successively with sodium thiosulfate solution and brine, then dried (MgSO4) and evaporated in vacuo. The resultant material was dissolved in methanol (60 mL) and treated with 40% aqueous NaOH solution (60 mL) then refiuxed for 2 h. The reaction mixture was cooled and extracted with DCM/MeOH (ratio 95:5), dried (MgSO4), filtered and evaporated in vacuo to give a crude solid. Purification by column chromatography gave 5-fluoro-4-iodo-li/1- indole as a pale brown solid (1.05 g, 39 %).NMR deltaH (300 MHz, CDCl3) 6.49-6.52 (m, IH), 6.95 (apparent dt, J = 0.4, 8.6, IH), 7.26-7.33 (m, 2H) and 8.35 (s, IH)., 310886-79-4

As the paragraph descriping shows that 310886-79-4 is playing an increasingly important role.

Reference£º
Patent; PIRAMED LIMITED; WO2007/122410; (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

1601-18-9, Methyl 2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Methyl-1 -hydro-indol-3-yl) acetate (0.71 g, 2 mmol) was dissolved in 10 mL of a solution of methylmagnesium bromide After water, methanol was added, and 3.5 mL of the above-mentioned hydroxylamine potassium (NH2OK) solution was added thereto. After 0.5 hours, methanol was distilled off, and the solution was acidified to pH 3-4 with 2 mol / L hydrochloric acid solution. The mixture was extracted with ethyl acetate and the combined ethyl acetate layer was washed with saturated brine, dried over anhydrous magnesium sulfate and evaporated to dryness to give The crude product was recrystallized from ethyl acetate to give 0.32 g of a white powder. Yield: 44%., 1601-18-9

The synthetic route of 1601-18-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Qingdao University; Zhang, Lei; Han, Yantao; Bian, Jiang; Zhang, Jian; Xu, Wenfang; (11 pag.)CN105418480; (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

168824-94-0, tert-Butyl 3,4-dihydro-1H-pyrido[3,4-b]indole-2(9H)-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Excess 1,3-dibromopropane and methyl 2-(4-hydroxyphenyl)acetate are reacted in ethanol to give compound 25.Compound 6 was dissolved in DMF,After pulling with NaH hydrogen,Add compound 25,The compound 26 is obtained by reacting at normal temperature.Compound 26 was dissolved in DCM.Join TFA,Reaction under ice bath conditions gave compound 27.

168824-94-0, The synthetic route of 168824-94-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Second Military Medical University; Liu Na; Sheng Chunquan; Jiang Yanjuan; Tu Jie; Li Zhuang; Dong Guoqiang; Wu Shanchao; (31 pag.)CN108623585; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.942-26-7,5-Chlorotryptamine hydrochloride,as a common compound, the synthetic route is as follows.,942-26-7

EXAMPLE 113 – PREPARATION of N-(2-(5-Chloro-1 H-indol-3-yl)ethyl)-4-(3- fluorophenoxy)benzamide. A solution of 4-(3-fluorophenoxy)benzoic acid(0.180 g, 0.775 mmol), 2-(5-chloro-1 H- indol-3-yl)ethanamine hydrochloride (0.180 g; 0.775 mmol), HATU (0.324 g; 0.852 mmol) and Nu,Nu-diisopropylethylamine (0.334mL; 1.94 mmol) in DMF (5 mL), was stirred at room temperature overnight. The reaction mixture was partitioned between ethyl acetate and sodium hydrogen sulfate, the organic layer was washed with sodium carbonate, brine, dried and concentrated under reduced pressure. The crude mixture was purified by flash chromatography on silica (eluent 2 to 20 % ethyl acetate in dichloromethane and 20 to 100% ethyl acetate in heptane ) to yield 0.065 g (20%) of the title compound as a white solid.ESI/APCI(+):409 (M+H); ESI/APCI(-): 407 (M-H).

942-26-7 5-Chlorotryptamine hydrochloride 2827494, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; KATHOLIEKE UNIVERSITEIT LEUVEN, K.U. LEUVEN R&D; REMYND; GRIFFIOEN, Gerard; VAN DOOREN, Tom; ROJAS DE LA PARRA, Veronica; ALLASIA, Sara; MARCHAND, Arnaud; KILONDA, Amuri; CHALTIN, Patrick; WO2012/80221; (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

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

To a solution of ethanol (50 mL) was added 1-methyl-5-nitro-1H-indole (2.6 g, 0.015 mol)Hydrazine hydrate (8.7 g, 0.15 mol),The resulting solution was cooled to zero,Then add NaneyNi dropwise.After completion of the dropwise addition, the mixture was stirred at room temperature for 6 hours.After filtration, the residue was purified by column chromatography (petroleum ether-ethyl acetate = 100/0-50/50) to give 1-methyl-1H-indol-5-amine

29906-67-0, The synthetic route of 29906-67-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Shanghai Hansoh BioMedical Co., Ltd.; Zhao, Zhiming; Deng, Xiangjun; Huang, Zhiqiang; Yu, Hongping; Xu, Yaocahng; Pan, Zhongzong; Bao, Rudi; (62 pag.)CN106349241; (2017); 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