Tag: M.W:100-200

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

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

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.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.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.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.244-69-9,5H-Pyrido[4,3-b]indole,as a common compound, the synthetic route is as follows.

Another reaction vessel was charged with 17.2 ml of 1,3-dibromobenzene, 6.0 g of 5H-pyrido[4,3-b]indole, 1.1 g of copper powder, 9.9 g of potassium carbonate, and 0.6 ml of dimethyl sulfoxide, followed by heating and stirring at 180C for 4 hours. After cooling to room temperature, 50 ml of chloroform was added thereto, the insoluble materials were removed by filtration and the filtrate was concentrated under reduced pressure to obtain a crude product. The crude product was purified by column chromatography (carrier: silica gel, eluent: hexane/chloroform) to obtain 7.1 g (yield 62%) of 5-(3-bromophenyl)-5H-pyrido[4,3-b]indole as a white powder., 244-69-9

As the paragraph descriping shows that 244-69-9 is playing an increasingly important role.

Reference£º
Patent; Hodogaya Chemical Co., Ltd.; EP2241568; (2010); 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.120-72-9,1H-Indole,as a common compound, the synthetic route is as follows.

To a solution of indole (10.021 g, 85 mmol) in diethyl ether (150 mL) was added oxalyl chloride (11.0 mL, 16.3 g, 0.13 mol) dropwise over 10 minutes and the yellow suspension was allowed to stir for a further 30 minutes at room temperature. Saturated aqueous sodium bicarbonate (20 mL) was then added with caution and the biphasic mixture was stirred for 16 hours. The product was then collected using vacuum filtration, washed with diethyl ether and dried overnight at 40 C to give a yellow solid (14.167 g, 88%): m.p. 193-196 C; (Lit. 210 C decomp.)47; numax/cm-1(KBr) 3549, 3195, 1719, 1611, 1268; deltaH(300 MHz, DMSO-d6) 7.26 [1H, ddd,J9.1, 7.1, 1.7, C(5)-H], 7.29 [1H, ddd,J9.3, 7.1, 1.9, C(6)-H], 7.52-7.58 [1H, m, C(7)-H], 8.14-8.20 [1H, m, C(4)-H], 8.42 [1H, d,J3.3, C(2)-H], 12.36 (1H, bs, N-H); m/z (ESI+) = 190.3 [(M+H)+100%]., 120-72-9

The synthetic route of 120-72-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Winfield, Hannah J.; Cahill, Michael M.; O’Shea, Kevin D.; Pierce, Larry T.; Robert, Thomas; Ruchaud, Sandrine; Bach, Stephane; Marchand, Pascal; McCarthy, Florence O.; Bioorganic and Medicinal Chemistry; vol. 26; 14; (2018); p. 4209 – 4224;,
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

5192-23-4, 4-Aminoindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of 4-chloro-5-[3-(2-chloroethoxy)phenyl]-nicotinonitrile (200 mg, 0.68 mmol), 4-aminoindole (135 mg, 1 mmol), DavePhos (80 mg, 0.20 mmol), and K3PO4 (216 mg, 1 mmol) in 4 mL anhydrous ethylene glycol dimethyl ether was added Pd2(dba)3 (62 mg, 0.07 mmol). The mixture was heated at 90 C. for 2 h then cooled, filtered through celite, concentrated in vacuo, and purified by flash chromatography on silica gel eluting with a gradient of 5-50% MeOH in CH2Cl2 to yield 155 mg (59% yield) of 5-[3-(2-chloroethoxy)phenyl]-4-(1H-indol-4-ylamino)-nicotinonitrile 165 as a tan solid. MS: 389.1 (M+H), HPLC retention time: 9.60 min.(a)., 5192-23-4

The synthetic route of 5192-23-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Cole, Derek Cecil; Boschelli, Diane Harris; Wang, Yanong Daniel; Asselin, Magda; Joseph-McCarthy, Diane Marie; Prashad, Amarnauth Shastrie; Wissner, Allan; Dushin, Russell; Wu, Biqi; Tumey, Lawrence Nathan; Niu, Chuan S.; Chen, Joan; US2007/287708; (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

51417-51-7,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.

General procedure: Under a nitrogen stream, 5-bromo-1H-indole (25g, 0.128mol), 4,4,4?,4?,5,5,5?,5?-octamethyl-2,2?-bi(1,3,2-dioxaborolane)(48.58g, 0.191mol), Pd (dppf) Cl2 (5.2g, 5mol), KOAc (37.55g, 0.383mol), and 1,4-dioxane (500ml) mixed, and the mixture was stirred for 12 hours at 130C .After completion of the reaction, and extracted with ethyl acetate, water was removed by MgSO4, column chromatography (hexane: EA = 10: 1 (v / v)) purified to at 5- (4,4,5,5-tetra to give methyl 1,3,2-dioxaborolan-2-yl)-lH-indole (22.32g, 72% yield).7-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indolewas obtained by performing the same procedure as in ofPreparation Example 1, except that 7-bromo-1H-indole was used insteadof 5-bromo-1H-indole.

The synthetic route of 51417-51-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DOOSAN CORPORATION; PARK, HO CHEOL; BAE, HYUNG CHAN; EUM, MIN SIK; BEAK, YOUNG MI; LEE, CHANG JUN; SHIN, JIN YONG; KIM, TAE HYUNG; (163 pag.)JP2015/528445; (2015); 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