Day: March 18, 2022

192189-07-4, tert-Butyl 3-iodo-1H-indole-1-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

192189-07-4, General procedure: First, Pd(OAc)2 (4.50 mg, 0.02 mmol), NaHCO3 (210 mg, 2.50 mmol), nBu4NCl (278 mg,1.00 mmol) and dry, degassed DMF (3 mL) were placed in an argon flushed screw-cap Schlenktube. Then, (hetero)aryl iodide 1 (1.00 mmol) and allyl alcohol (2) (1.5 mmol) were added (forexperimental details, see Table 2). The mixture was placed in an oil bath at 50 C and was stirreduntil the educt had disappeared as monitored by TLC. After cooling to room temperature, MgO(75.0 mg, 1.86 mmol), PPh3, (262 mg, 1.00 mmol) and ethyl bromoacetate (167 mg, 1.00 mmol)were subsequently added to the reaction mixture and was heated to 50 C for the time t2. Aftercompletion of the sequence the crude reaction mixture was allowed to cool to room temperatureand diluted with ethyl acetate and extracted three times with water. The organic phase was driedwith anhydrous magnesium sulfate and adsorbed on Celite during evaporation. Then, theproduct was purified by chromatography on silica gel (n-hexane/ethyl acetate) to afford theanalytically pure 5-(hetero)arylpent-2-enoates 4.

As the paragraph descriping shows that 192189-07-4 is playing an increasingly important role.

Reference：
Article; Panther, Jesco; Roehrich, Adalbert; Mueller, Thomas J. J.; ARKIVOC; vol. 2012; 3; (2012); p. 297 – 311;,
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.16732-69-7,Ethyl 7-bromo-1H-indole-2-carboxylate,as a common compound, the synthetic route is as follows.

EXAMPLE XVIII 7-bromo-1-methyl-1H-indole-2-carboxylic acid 7.37 g ethyl 7-bromo-1H-indole-2-carboxylate are dissolved in 50 ml N,N-dimethylformamide, cooled to 0 C. and combined with 1.16 g sodium hydride (60% in mineral oil). The mixture is stirred for 20 minutes and then 1.78 ml methyl iodide are added dropwise. Then the mixture is allowed to come up to ambient temperature and stirred for 12 hours. Then 80 ml of methanol and 27.5 ml 2 N sodium hydroxide solution are added and the mixture is stirred for 3 hours at ambient temperature. The methanol is eliminated in vacuo, the residue is mixed with water and the precipitate is suction filtered. The filtrate is washed twice with ethyl acetate and the aqueous phase is combined with sufficient 2 N hydrochloric acid to give a pH of 2. The precipitated solid is suction filtered, washed with water and dried. Yield: 4.26 g (61% of theory) Mass spectrum (ESI-): m/z=252 [M-H]-

16732-69-7, The synthetic route of 16732-69-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; US2011/269737; (2011); 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

31241-19-7, 5-Methoxy-2,3,3-trimethyl-3H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Following a modified procedure [22], to a mixture of various substituted 2,3,3-trimethylindole (7.0 mmol), 2-formylpyrrole (1.78 g, 14 mmol), piperidine (12 mL,14 mmol) and ice acetic acid (16.5 mL, 21 mmol) in toluene (50 mL) were addedunder a Dean-Stark trap condition and the mixture was refluxed for 3 h. Thecompletion of the reaction was confirmed by TLC. The brown dark reaction mixturewas cooled, concentrated and separated by column chromatography. The correspondingproducts NDABs as a solid were obtained., 31241-19-7

As the paragraph descriping shows that 31241-19-7 is playing an increasingly important role.

Reference：
Article; Li, Yujiao; Yan, Jiaying; Cheng, Kai; Kong, Shuai; Zheng, Kaibo; Wang, Long; Zhang, Nuonuo; Research on Chemical Intermediates; vol. 43; 10; (2017); p. 5337 – 5344;,
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

31241-19-7, 5-Methoxy-2,3,3-trimethyl-3H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of compound 2 in dichloromethane (30 mL) at 0 C was added dropwise 2 equivalents of 1 M BBr3 in dichloromethane and the mixture was stirred at room temperature for 12 h. Upon the completion of reaction as monitored by thin layer chromatography (TLC), the reaction mixture was washed with saturated aqueoussolution of sodium bicarbonate and the organic extracts were driedover Na2SO4, filtered, and evaporated to afford 3 as a brown solid in79% yield

31241-19-7, As the paragraph descriping shows that 31241-19-7 is playing an increasingly important role.

Reference：
Article; Saikiran, Maryala; Sato, Daisuke; Pandey, Shyam S.; Ohta, Takeshi; Hayase, Shuzi; Kato, Tamaki; Dyes and Pigments; vol. 140; (2017); p. 6 – 13;,
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

6127-19-1,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.6127-19-1,6-Bromo-2-methyl-1H-indole,as a common compound, the synthetic route is as follows.

General procedure: An appropriate amount 2,3-dichloro-1,4-naphthoquinone 1and the corresponding nucleophile were stirred in dichloromethane (30 mL) with Na2CO3(1.56 g) solution for 2-3 h at room temperature. The color of the solution quickly changedand the reaction was monitored by TLC. Chloroform (30 mL) was added to the reactionmixture. The organic layer was washed with water (4 × 30 mL), and dried over Na2SO4.After the solvent was evaporated the residue was purified by column chromatography onsilica gel.

As the paragraph descriping shows that 6127-19-1 is playing an increasingly important role.

Reference：
Article; Ibis, Cemil; Ayla, Sibel Sahinler; Bahar, Hakan; Stasevych, Maryna V.; Komarovska-Porokhnyavets, Olena; Novikov, Volodymyr; Phosphorus, Sulfur and Silicon and the Related Elements; vol. 190; 9; (2015); p. 1422 – 1433;,
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

289483-82-5, 4-Methyl-7-nitro-1H-indole-3-carbonitrile is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of the above residue in MeOH (25 mL) was added Pd/C (100 mg, 20% w/w). After stirring at room temperature under 1 atm Lh for 3 h, the reaction mixture was filtered. The resulting solution was concentrated under reduced pressure. The residue was purified by flash column chromatography to give Sl-4 (208 mg, 1.18 mmol, 48% yield over two steps)., 289483-82-5

289483-82-5 4-Methyl-7-nitro-1H-indole-3-carbonitrile 11622527, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; DANA-FARBER CANCER INSTITUTE, INC.; GRAY, Nathanael S.; FISCHER, Eric; YOON, Hojong; ZHANG, Tinghu; FAUST, Tyler; DONOVAN, Katherine; CAI, Quan; (84 pag.)WO2019/147783; (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

1065181-58-9, Ethyl 5-bromo-1H-indole-7-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 80:Ethyl 5-Bromo-3-[2-(1 -methylethyl)tetrahydro-2H-thiopyran-4-yl]-1 H-indole-7- carboxylate.2-(1-methylethyl)tetrahydro-2H-thiopyran-4-one (1.185 g, 7.49 mmol) was dissolved in dry dichloromethane (DCM) (20 ml_), cooled in an ice bath to ca 0 0C, and stirred under argon. Trimethylsilyl trifluoromethanesulfonate (2.71 ml_, 14.98 mmol) was added dropwise over 10 minutes, and dry DCM (5 ml.) was used to wash in the last of the trimethylsilyltrifuoromethanesulfonate. To this mixture was added dropwise, a solution of ethyl 5-bromo-1 H-indole-7-carboxylate (2.145 g, 8 mmol) in dry DCM (20 ml_), and then an additional portion of dry DCM (5 ml.) was used to wash the last of ethyl 5-bromo-1 H- indole-7-carboxylate into the reaction. Triethylsilane (4.77 ml_, 30.0 mmol) was added to the reaction in one portion. The resulting mixture was stirred 2h at 0 0C, and left stirring at 23 0C overnight. The reaction was diluted with saturated aqueous sodium bicarbonate, and the resulting biphasic mixture was extracted with DCM, dried (MgSO4) and the DCM was removed in vacuo to give the title compound as a dark yellow oil. LC/MS: m/z 414.3 (M+H), Rt 1.58 min.

1065181-58-9, The synthetic route of 1065181-58-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; SMITHKLINE BEECHAM CORPORATION; WO2008/118724; (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.162100-95-0,6-Fluoro-5-methyl-1H-indole,as a common compound, the synthetic route is as follows.,162100-95-0

A solution of 6-fluoro-5-methyl-1 H-indole [CAS 162100-95-0] (1 .7 g, 1 1 .4 mmol) in CH2CI2 (100 mL) was cooled to 0C under N2-atmosphere. A solution of diethylalunninunn chloride 1 M in hexane (17.1 mL, 17.1 mmol) was added dropwise and the resulting mixture was kept at 0C for 15 min. A solution of 2-(4-chloro- 2-methoxyphenyl)acetyl chloride 1a (3.50 g, 16 mmol) in CH2CI2 (50 mL) was added dropwise. Stirring was continued at 0C for 1 h and at room temperature for 2 h. The reaction mixture was poured out in a stirring ice/Rochelle salt solution. After the ice had melted, the mixture was filtered over dicalite and the filter cake was washed several times with THF. The filtrates were combined. The layers were separated and the organic layer was washed with brine, dried over MgSO4, filtered and evaporated under reduced pressure. The solid residue was suspended in CH2CI2 (30 ml_), the precipitate was filtered off and dried under vacuum at 50C to provide 2-(4-chloro-2-methoxyphenyl)-1 -(6-fluoro-5-methyl-1 H-indol-3-yl)ethanone 7a (2.76 g).

As the paragraph descriping shows that 162100-95-0 is playing an increasingly important role.

Reference：
Patent; JANSSEN PHARMACEUTICALS, INC.; KATHOLIEKE UNIVERSITEIT LEUVEN; KESTELEYN, Bart, Rudolf, Romanie; BONFANTI, Jean-Francois; JONCKERS, Tim, Hugo, Maria; RABOISSON, Pierre, Jean-Marie, Bernard; BARDIOT, Dorothee, Alice, Marie-Eve; MARCHAND, Arnaud, Didier, M; (68 pag.)WO2016/180696; (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

1059630-08-8, (4aS,9bR)-Ethyl 6-bromo-3,4,4a,5-tetrahydro-1H-pyrido[4,3-b]indole-2(9bH)-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1.000 equivalents of ethyl (4aS,9bR)-6-bromo-l,3,4,4a,5,9b-hexahydro-2H- pyrido[4,3-b]indole-2-carboxylate is charged into a reactor with 0.50 volumes of dimethylacetamide solvent at 20 C. A solution of 1.500 equivalents of N-methyl chloroacetamide in 0.30 volumes of dimethylacetamide is added, followed by 1.000 equivalents of potassium iodide, and 1.700 equivalents of diisopropylethylamine. The resulting suspension is heated at 102 C for 15 to 18 hours. After cooling to 45 C, 5.00 volumes of water are added. After further cooling and agitation, the product is isolated as a solid filter cake and is washed with additional water and dried under vacuum., 1059630-08-8

1059630-08-8 (4aS,9bR)-Ethyl 6-bromo-3,4,4a,5-tetrahydro-1H-pyrido[4,3-b]indole-2(9bH)-carboxylate 59317960, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; INTRA-CELLULAR THERAPIES, INC.; LI, Peng; ZHANG, Qiang; (113 pag.)WO2019/241278; (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

1245643-61-1, Methyl 5-chloro-1H-indole-6-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of methyl 5-chloro-1 /-/-indole-6-carboxylate (500 mg, 2.39 mmol), B0C2O (781 mg, 3.58 mmol) and DMAP (58.3 mg, 0.477 mmol) in MeCN (8 mL) was stirred at room temperature for 16 h then concentrated in vacuo. The crude product was purified by fee (24 g, 0-50% EtOAc in isohexane) to return the title compound (737 mg, quant) as a colourless oil, which solidified on standing. LCMS [M+H]+ 310; 1 H NMR (400MHz, DMSO-d6) delta 8.59 (s, 1 H), 7.91 (d, J = 3.1 Hz, 1 H), 7.86 (s, 1 H), 6.77 (dd, J = 3.7, 0.7 Hz, 1 H), 3.88 (s, 3H), 1.63 (s, 9H).

1245643-61-1, As the paragraph descriping shows that 1245643-61-1 is playing an increasingly important role.

Reference：
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; JORDAN, Allan; NEWTON, Rebecca; (174 pag.)WO2017/178844; (2017); 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