Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.399-51-9,6-Fluoro-1H-indole,as a common compound, the synthetic route is as follows.

Place 40 ml DMF in a round bottom flaskSlowly add 6.89 ml of POCl3 (phosphorus oxychloride) under ice bath.After dropping,After stirring in an ice bath for 35 minutes,At a constant pressure dropping funnel was slowly added 5g6- fluoro indole in DMF,Stir at 35 C for 40 min.The reaction solution gradually changed from colorless to red.TLC shows that after the reaction is completed,Add 100ml of 19.3mmol/L aqueous NaOH,Stir vigorously for 30 minutes at 80C.Cool the reaction solutionAdd ethyl acetate extraction,30ml each time,A total of three extractions.Organic layers merge,After drying over anhydrous sodium sulfate,Evaporated to drynessSilica gel column chromatography 4.5g Intermediate I-1 (white solid, yield75%)., 399-51-9

The synthetic route of 399-51-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Chinese Academy Of Sciences Shanghai Pharmaceutical Institute; Hu Youhong; Geng Meiyu; Xing Weiqiang; Ding Jian; Ai Jing; (86 pag.)CN103664895; (2018); 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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2795-41-7,6-Fluoroindole-3-carboxaldehyde,as a common compound, the synthetic route is as follows.

General procedure: A mixture of glyoxalylhydrazide 18 (1.47mmol) and aldehyde 20 or 22 (1.47mmol) in ethanol (5mL) was refluxed for 6h. After completion of the reaction, ethanol was distilled off and the residue was taken into water (10mL) and allowed to stir at room temperature for 30min. The obtained suspension was filtered, washed with water and dried to obtain yellow solid ketohydrazide-hydrazones 21a-o and 23a-e in 88-96% yields., 2795-41-7

2795-41-7 6-Fluoroindole-3-carboxaldehyde 262903, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Article; Tantak, Mukund P.; Klingler, Linus; Arun; Kumar, Anil; Sadana, Rachna; Kumar, Dalip; European Journal of Medicinal Chemistry; vol. 136; (2017); p. 184 – 194;,
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.935269-27-5,3-Oxoisoindoline-4-carboxylic acid,as a common compound, the synthetic route is as follows.

935269-27-5, Compound 16f was coupled with 4-methoxyaniline using a coupling agent such as EDCI in DMF to give 3-oxo-2,3-dihydro-lH-isoindole-4-carboxylic acid (4- methoxy-phenyl)-amide Compound 16g 1H NMR (300 MHz, MeOD) 3.80 (s, 3H), 4.56 (s, 2H), 6.94 (d, J = 9 Hz, 2H), 7.70 (d, J = 9 Hz, 2H), 7.78 (m, 2H), 8.40 (m, IH); MS (ESI) m/z: 283 (MH+).

The synthetic route of 935269-27-5 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; JANSSEN PHARMACEUTICA, N.V.; WO2007/47646; (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

343-90-8, 1-(5-Fluoro-1H-indol-3-yl)-N,N-dimethylmethanamine is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a stirred mixture of S1 (R = H, F, Br, or OMe; 5.20 mmol) and diethyl malonate (4.85 mmol) in Et2O (2.6mL) was added dropwise ethyl propiolate (5.20 mmol) at room temperature. The mixture was stirred for 45 min atthis temperature, followed by quenching with H2O. The whole was extracted with Et2O. The extract was washedsuccessively with H2O and brine, and dried over MgSO4. The filtrate was concentrated under reduced pressure togive an oily residue, which was purified by flash chromatography over silica gel with n-hexane-EtOAc (8:1) togive the corresponding S2 as a pale yellow needle., 343-90-8

The synthetic route of 343-90-8 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Iwata, Akira; Inuki, Shinsuke; Oishi, Shinya; Fujii, Nobutaka; Ohno, Hiroaki; Tetrahedron; vol. 71; 37; (2015); p. 6580 – 6585;,
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

2532-74-3, 2-(1-Methyl-1H-indol-3-yl)ethanol is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 3.64 g 1-methyl-3-(2-hydroxyethyl)indole, 18 g methyltriphenoxyphosphonium iodide (J.O.C. 35 2323) and 75 ml dry N,N-dimethylformamide is stirred 2.5 hours at room temperature. Then 5 ml methanol are added, and the mixture is stirred 30 minutes. The mixture is poured into 500 ml dichloromethane and is washed successively with 50 ml portions of 5% aquous sodium thiosulfate, 10% NaOH, and water. The organic layer is dried briefly over magnesium sulfate and most of the solvent removed by evaporation, affording 1-methyl-3-(2-iodoethyl)indole., 2532-74-3

The synthetic route of 2532-74-3 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Syntex (U.S.A.) Inc.; US4255432; (1981); 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

10601-19-1, 5-Methoxy-1H-indole-3-carbaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The relevant indole-3-carboxaldehyde (2a-c, 10 mmol) in THF(25 mL) was added dropwise to a stirred solution of NaH (25 mmol)in THF (25 mL) at 0 C and CH3I (13.2 mmol) was added after 15 minstirring. The reaction mixturewas moved to room temperature andstirred for further 24 h. Then the solvent was removed in vacuumand the residue was extracted by ethyl acetate. The organic layerwas washed with brine, dried over anhydrous sodium sulfate,filtered and concentrated in vacuum. Recrystallization affordedcompound 3a-c with yields of 93.4-97.5%., 10601-19-1

As the paragraph descriping shows that 10601-19-1 is playing an increasingly important role.

Reference：
Article; Chen, Kun; Zhang, Ya-Liang; Fan, Jing; Ma, Xiang; Qin, Ya-Juan; Zhu, Hai-Liang; European Journal of Medicinal Chemistry; vol. 156; (2018); p. 722 – 737;,
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.1204-32-6,Methyl 1-Methylindole-6-carboxylate,as a common compound, the synthetic route is as follows.

Step 2: 1-Methyl-lH-indole-6-carboxylic acid (167) [0334] Methyl 1-METHYL-LH-INDOLE-6-CARBOXYLATE 166 (1.24 MMOL) was stirred with sodium hydroxide (0.59g, 14.88 MMOL) in a 2: 2: 1 mixture of methanol/THF/water (7.5 mL) for 36 hrs at rt to form a precipitate which was collected by filtration and LYOPHILIZED overnight to give the title compound 167 (0.54g, 99percent yield). MS: 175.06 (CALC), 176.1 (OBS).

1204-32-6, The synthetic route of 1204-32-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; METHYLGENE, INC.; WO2005/30704; (2005); 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.90924-06-4,1-Methyl-4-indolecarboxylic Acid,as a common compound, the synthetic route is as follows.,90924-06-4

Example 11 O-(7-azabenzotriazol-1-yl)-N,N,N’,N’-tetramethyluronium hexafluorophosphate (113 mg), diisopropylethylamine (0.127 mL), and 4-dimethylaminopyridine in a catalytic amount were added to a mixture of N-cyclopropyl-5,6,7,8-tetrahydrocinnolin-6-amine monohydrochloride (56 mg), 1-methyl-1H-indole-4-carboxylic acid (52 mg), and DMF (2 mL) under an argon gas atmosphere, followed by stirring under heating for 60 hours at an oil temperature of 60 C., and then the resultant was cooled to room temperature. The reaction liquid was diluted with ethyl acetate and then washed with water (3 times) and saturated brine in this order, followed by drying, and concentrating under reduced pressure. The residue was purified by silica gel column chromatography (chloroform/methanol), thereby obtaining N-cyclopropyl-1-methyl-N-(5,6,7,8-tetrahydrocinnolin-6-yl)-1H-indole-4-carboxamide (9.3 mg).

As the paragraph descriping shows that 90924-06-4 is playing an increasingly important role.

Reference：
Patent; ASTELLAS PHARMA INC.; Kawakami, Shimpei; Sakurai, Minoru; Kawano, Noriyuki; Suzuki, Takayuki; Shiraishi, Nobuyuki; Hamaguchi, Wataru; Sekioka, Ryuichi; Moritomo, Hiroyuki; Motitomo, Ayako; US2014/249151; (2014); 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

1469-48-3, cis-3a,4,7,7a-Tetrahydro-1H-isoindole-1,3(2H)-dione is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

a Cis-Octahydroisoindole Cis-4-cyclohexene-1,2-dicarboximide (10.9 g) was hydrogenated over 10% palladium on carbon (1 g) in absolute ethanol (420 ml) at 50 psi for 10 minutes. The mixture was filtered then evaporated to give cis-cyclohexane-1,2-dicarboximide (10.6 g). To anhydrous diethyl ether (200 ml) was cannulated under nitrogen a 1M diethyl ether solution (200 ml) of lithium aluminium hydride.

1469-48-3, As the paragraph descriping shows that 1469-48-3 is playing an increasingly important role.

Reference：
Patent; Merck Sharp & Dohme, Ltd.; US5618812; (1997); 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.1008-07-7,7-Chloro-1H-indole-3-carbaldehyde,as a common compound, the synthetic route is as follows.

We heated a mixture of (1-6) (1 mmol) and l-methylimidazol-255(l,3H)- dione (which we synthesized according to the method used by Janin et al., Eur. J. Org. Chem. 2002:1763-1769, 2002) (250mg, 2.5 mmol) in piperidine (2 mL) at 1100C for four hours under an argon atmosphere. Then, we allowed the reaction mixture to cool in a refrigerator (~ 5C) with the addition of ether (2 mL). We filtered the precipitate and washed it with ether to give (1-7). 1H NMR (500 MHz, DMSO-d6): delta 12.15 (IH, br s), 10.26 (IH, br s), 8.23 (IH, s), 7.79 (IH, d, J = 8.0 Hz), 7.27 (IH, d, J = 8.0 Hz,), 7.13 (IH, t, J = 7.8 Hz), 6.82 (IH, s), 2.97 (3H, s).

1008-07-7, The synthetic route of 1008-07-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; PRESIDENT AND FELLOWS OF HARVARD COLLEGE; THE BRIGHAM AND WOMEN’S HOSPITAL, INC.; WO2007/75772; (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