Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.387-44-0,7-Fluoroindole,as a common compound, the synthetic route is as follows.,387-44-0

7-fluoro-1 H-indole (0.200 g),2,6-Bis (trifluoromethyl) benzoyl chloride (0.368 g)Was dissolved in dichloromethane (6 mL)After addition of zirconium (IV) chloride (0.517 g) under ice cooling,And the mixture was stirred at room temperature for 2 hours.Water was added to the reaction mixture under ice cooling, followed by extraction with ethyl acetate, and the organic layer was washed with saturated brine. The organic layer was dried over anhydrous sodium sulfate, concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (ethyl acetate / hexane) to give the title compound (0.234 g) as a colorless oil .

387-44-0 7-Fluoroindole 2774504, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; DAIICHI SANKYO COMPANY LIMITED; NAGAMOCHI, MASATOSHI; KOZAWA, YUJI; INAGAKI, HIROAKI; GOTANDA, KENTOKU; NOGUCHI, TETSUJI; TORIHATA, MUNEFUMI; YOSHINO, TOSHIHARU; ISOBE, TAKASHI; (113 pag.)JP2016/141632; (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

5654-93-3, 3-Methyl-7-azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5654-93-3

Example 19A 3-Methyl-1H-pyrrolo[2,3-b]pyridine 7-oxide A little at a time, 3.00 g (22.70 mmol) of 3-methyl-1H-pyrrolo[2,3-b]pyridine (Hands, David; Bishop, Brian; Cameron, Mark; Edwards, John S.; Cottrell, Ian F.; Wright, Stanley H. B.; Synthesis 1996, 877-882.) are added to a solution of 10.45 g (45.40 mmol) of meta-chloroperoxybenzoic acid in 250 ml of dichloromethane, and the mixture is stirred at 10 C. for 2 h. Addition of methanol gives a clear solution which is subjected directly to column chromatography on silica gel (mobile phase: dichloromethane/methanol 100:4 to 3:1). A further purification step by preparative HPLC yields the target compound. Yield: 1.4 g (42% of theory) LC-MS (Method 3): Rt=1.22 min. MS (ESI pos.): m/z=149 [M+H]+. 1H-NMR (DMSO-d6, 400 MHz): delta=2.25 (s, 3H), 7.05 (dd, 1H), 7.22 (s, 1H), 7.60 (d, 1H), 8.10 (d, 1H), 11.97 (br. s, 1H).

The synthetic route of 5654-93-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Bayer HealthCare AG; US2008/269268; (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.169674-02-6,4-Chloro-5-fluoro-1H-indole,as a common compound, the synthetic route is as follows.

a) A suspension of 0.11 g of sodium hydride dispersion in 15 ml of tetrahydrofuran was treated with 0.5 g of 4-chloro-5-fluoroindole at 0 and stirred at this temperature for 1 hour. After the addition of 0.4 ml of (S)-methyloxirane the reaction mixture was stirred at s room temperature for 48 hours and subsequently treated with water. The mixture was diluted with ether, washed with water and with saturated sodium chloride solution and the organic phase was dried over sodium sulfate. After removal of the solvent the residue was chromatographed over 30 g of silica gel with toluene-ethyl acetate (33:1). There was obtained 0.53 g (78.9%) of (S)-1-(4-chloro-5-fluoro-indol-1-yl)-propan-2-ol as a yellow oil., 169674-02-6

As the paragraph descriping shows that 169674-02-6 is playing an increasingly important role.

Reference£º
Patent; Hoffmann-La Roche Inc.; US5494928; (1996); 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

272-49-1, 4-Azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Azaindole (2.0 g, 16.93 mmol) was added to aluminum chloride (11.29 g, 85 mmol) in dry dichloromethane (85 mL) at 0 ¡ãC under argon atmosphere. After 30 mm ato ¡ãC, the mixture was warmed to room temperature and ethyl chlorooxoacetate (11.56 g,85 mmol) was added dropwise. The reaction mixture was stirred vigorously forovernight, then carefully ice was added. Adjust pH to 7 with 4 N NaOH then cold sat.NaHCO3 solution. The product was extracted with DCM 3 times, dried over Na2SO4,filtered, and concentrated to afford ethyl 2-oxo-2-(1H-pyrrolo[3,2-bjpyridin-3-yl)acetateas a yellow oily residue. After a washing with cold petroleum ether the title compound was obtained as a light yellow powder 280 mg (7.6percent). ESI-MS(-): MS m/z 217.1., 272-49-1

272-49-1 4-Azaindole 9226, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; MILLER, Michael Matthew; ALLEN, Martin Patrick; LI, Ling; BOWSHER, Michael S.; GILLIS, Eric P.; MULL, Eric; ZHAO, Qian; SUN, Li-Qiang; LANGLEY, David R.; SCOLA, Paul Michael; (214 pag.)WO2017/176608; (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

15861-24-2, Indole-5-carbonitrile is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 5-cyano indole (100 g) in dichloromethane (4 L) titanium tetrachloride (214 g) was added at 0-5 C. under nitrogen atmosphere. The resulting mixture was stirred for 45 minutes and then 4-chlorobutyryl chloride (168.8 g) was added to the mixture drop wise. The reaction mass was stirred at room temperature for 5 hours and again cooled to 0-5 C. The reaction mass is quenched by ice-cold water (2 L) and stirred for 4 hours. The resulting solid material was filtered, washed with water (300 mL). Water (1 L) was added to the wet material and the pH of the reaction mass was adjusted to 7.0 with aqueous solution of sodium bicarbonate (3% w/v). The reaction mass was stirred for 10-15 minutes at room temperature, filtered, washed with water and dried to provide the desired compound. [0506] Yield: 120 g (69%) [0507] Purity (by HPLC): 91.96%., 15861-24-2

15861-24-2 Indole-5-carbonitrile 27513, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; Iqbal, Javed; Oruganti, Srinivas; Rapolu, Rajesh Kumar; Peddy, Vishweshwar; Boge, Rajesham; Pathivada, Deepika; Velaga, Dharma Jagannadha Rao; Yarraguntla, Sesha Reddy; Baddam, Sudhakar Reddy; Naredla, Anitha; Doniparthi, Kiran Kumar; Nadgoud, Ramesh Kumar; Pagadala, Narasimha Rao; Unniaran, Syam Kumar; Ramakrishnan, Srividya; US2015/126525; (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.348640-06-2,4-Bromo-7-azaindole,as a common compound, the synthetic route is as follows.

To a solution of 4-bromo- l77-pyrrolo[2,3-b]pyridine (200 mg, 1.02 mmol) in DMF (3 mL) was added NaH (49 mg, 2.0 mmol, 60% in mineral oil) at 0 C. Then to the mixture was stirred at 0 C for 30 min. And then Mel (290 mg, 2.04 mmol) was added to the above mixture at 0 C, then the mixture was stirred at 25 C for 15.5 h. TLC showed the reaction was completed. The resulting mixture was concentrated under reduced pressure. The residue was poured into water (50 mL) and stirred at 0 C for 30 min. The aqueous phase was extracted with EtOAc (50 mL x3). The combined organic phase was washed with brine (50 mL), dried over Na2S04, filtered and concentrated in vacuum. The residue was purified by Combi Flash (10% EtOAc in pentane) to give 4-bromo- 1 -methyl- 1 //-pyrrolo| 2.3-b Ipyridine (180 mg, yield: 84%) as yellow oil. NMR (400 MHz, CDCb) d 3.89 (3H, s), 6.49 (1H, d, J= 3.6 Hz), 7.20-7.25 (1H, m), 7.26 (1H, d, J= 2.4 Hz), 8.13 (1H, d, J= 5.2 Hz)., 348640-06-2

The synthetic route of 348640-06-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PETRA PHARMA CORPORATION; KESICKI, Edward A.; RAVI, Kannan Karukurichi; LINDSTROeM, Johan; PERSSON, Lars Boukharta; LIVENDAHL, Madeleine; VIKLUND, Jenny; GINMAN, Tobias; FORSBLOM, Rickard; RAHM, Fredrik; HICKEY, Eugene R.; DAHLGREN, Markus K.; GERASYUTO, Aleksey I.; (478 pag.)WO2019/126733; (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

31827-04-0, Methyl 3-hydroxy-1H-indole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 184C Methyl 3-isopropoxy-1H-indole-2-carboxylate A solution of potassium tert-butoxide (0.25 g, 2.2 mmol) in DMSO (3 mL) at 0 C. was treated with a solution of Example 184B (0.3 g, 1.57 mmol) in DMSO (5 mL), warmed to room temperature, stirred for 1 hour, treated with 2-bromopropane (0.24 mL, 2.5 mmol), stirred at for 16 hours, and poured into ice/water (30 mL). The precipitate was filtered, washed with water and dried under vacuum at room temperature to provide the desired product (58%). MS (ESI(-)) m/e 232 (M-H)-; 1H NMR (300 MHz, DMSO-d6) delta 1.28 (d, 6H), 3.85 (s, 3H), 4.42-4.52 (m, 1H), 7.04 (t, 1H), 7.25 (t, 1H), 7.36 (d, 1H), 7.59 (d, 1H), 11.30 (s, 1H).

31827-04-0, The synthetic route of 31827-04-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BaMaung, Nwe Y.; Craig, Richard A.; Kawai, Megumi; Wang, Jieyi; Dai, Yujia; Guo, Yan; Sheppard, George; Verzal, Mary K.; Vasudevan, Anil; Michaelides, Michael; US2002/91148; (2002); 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.4769-96-4,6-Nitro-1H-indole,as a common compound, the synthetic route is as follows.

Camphorsulfonic acid (CSA) (6.9 mg, 0.03 mmol), the indolederivative (0.30 mmol) and hypervalent iodine reagent (119.4 mg,0.33 mmol) were placed into an oven-dried sealed bomb equippedwith a stirring bar under Ar. Under a positive ow of argon, 1.5 mLof freshly distilled 1,2-dichloroethane was added. The reaction wasstirred at 40 8C and monitored by 19F NMR spectroscopy until thedisappearance of the electrophilic triuoromethylthiolating re-agent 3 (typically 24 h). 15 mL of brine and 10 mL of CH2Cl2 wasadded and the organic phase was separated. The aqueous phasewas extracted with CH2Cl2 (3 10 mL) and the combined organicextracts were dried over anhydrous Na2SO4, and concentrated in vacuo. 3-(Triuoromethylthio)-1H-indole-5-carbonitrile (Table 2, en-try 11). Yield 78%, yellow solid, m.p. 156-158 8C. 1H NMR(400 MHz, ACETONE-D6, 293 K, TMS) d 11.43 (s, 1H), 7.98 (s,1H), 7.93 (d, J = 2.8 Hz, 1H), 7.61 (dd, J = 8.4, 0.8 Hz, 1H), 7.44 (dd,J = 8.4, 1.6 Hz, 1H) ppm; 19F NMR (376.4 MHz, ACETONE-D6) d45.70 (s, 3F) ppm; 13C NMR (100.7 MHz, ACETONE-D6, 293 K,TMS) d 138.53, 137.14, 131.01 (q, J = 309.6 Hz), 129.39, 125.61,123.74, 119.51, 113.87, 104.60, 94.22 (q, J = 2.5 Hz) ppm. MS (EI):m/z (%) 242, 173 (1 0 0). HRMS: Calculated for C10H5N2F3S:242.0126; Found: 242.0128.

4769-96-4, 4769-96-4 6-Nitro-1H-indole 78502, aindole-building-block compound, is more and more widely used in various.

Reference£º
Article; Ma, Bingqing; Shao, Xinxin; Shen, Qilong; Journal of Fluorine Chemistry; vol. 171; (2015); p. 73 – 77;,
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.16096-32-5,4-Methyl-1H-indole,as a common compound, the synthetic route is as follows.

General procedure: A 50 mL round bottom flask equipped with a magnetic stirring bar was charged with substituted indole 1 (1.0 mmol, 1.0 equiv), HMTA (2.0 mmol, 0.2803 g, 2.0 equiv), activated carbon (0.1 g) and DMF (2 mL). Then I2 (0.2 mmol, 0.0507g, 20 mol%) was added and the flask was equipped with a reflux condenser. The reaction mixture was stirred at 120 oC under open air and monitored by TLC. Upon completion of the reaction, the reaction mixture was cooled to room temperature. The resultant mixture was filtered through a pad of celite and the filter cake was washed thoroughly with EtOAc (4 ¡Á 6 mL). The filtrate was washed with 0.5 M aqueous HCl (10 mL), saturated NaHCO3 solution (10 mL) and saturated NaCl solution ( 10 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by flash column chromatography on silica gel eluted with hexane and ethyl acetate to give the product., 16096-32-5

The synthetic route of 16096-32-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Wang, Qing-Dong; Yang, Jin-Ming; Fang, Dong; Ren, Jiangmeng; Zeng, Bu-Bing; Tetrahedron Letters; vol. 58; 30; (2017); p. 2877 – 2880;,
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

53590-58-2, (6-Chloro-1H-indol-2-yl)methanol is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,53590-58-2

To (6-chloro-1H-indol-2-yl)-methanol (37.7 mmol) in THF at 0 C. was added manganese (IV) oxide and the mixture was stirred at room temperature for 16 h. The mixture was filtered over celite and rinsed with THF and EtOAc and evaporated to near dryness. The solid was filtered and washed with cold EtOAc/hex to give 6-chloro-1H-indole-2-carbaldehyde (62%, 2 steps).

53590-58-2 (6-Chloro-1H-indol-2-yl)methanol 16115151, aindole-building-block compound, is more and more widely used in various.

Reference£º
Patent; Wyeth; US2008/9485; (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