Category: 166104-20-7

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬ COA of Formula: C13H16N2O2, Which mentioned a new discovery about 166104-20-7

Mild deprotection of tert-butyl carbamates of NH-heteroarenes under basic conditions

Aqueous methanolic potassium carbonate under reflux has been demonstrated to be a highly effective deprotective agent for the tert -butyl carbamates of indoles, indazoles, carbazole, thiazoloindole, and pyrrole. The method is a mild one and is particularly expeditious for NH-heteroarenes bearing electron-withdrawing groups. Copyright Taylor & Francis Group, LLC.

Because enzymes can increase reaction rates by enormous factors and tend to be very specific, COA of Formula: C13H16N2O2, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 166104-20-7

Reference£º
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.166104-20-7,1-Boc-5-Aminoindole,as a common compound, the synthetic route is as follows.

Example 1; (A) A solution of the N-Boc protected amine (1 mmol) in TFE (2,2,2-trifluoroethanol) or HFIP (hexafluoroisopropanol) (5 mL) was placed in a sealed microwave vial. The reaction mixture was heated (100¡ãC or 150¡ãC) in a Biotage – Initiator.(TM). Sixty microwave reactor with stirring until the disappearance of the starting material was observed. After cooling to room temperature, the mixture was evaporated to dryness under reduced pressure. The crude product was purified by flash-column chromatography. 1H NMR and 13C NMR were measured on Bruker Avance DPX-300 NMR or Bruker Avance-300 NMR spectrometers, operating at a proton (1H) frequency of 300.13 MHz and carbon (13C) frequency of 75.43 MHz.Example 2 Following the procedure set forth in Example 1(A) above, indole derivatives were deprotected using TFE or HFIP in a microwave reactor at 150¡ãC as set forth in Table 1 below.

166104-20-7, 166104-20-7 1-Boc-5-Aminoindole 11593831, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; F. Hoffmann-La Roche AG; EP2070899; (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.166104-20-7,1-Boc-5-Aminoindole,as a common compound, the synthetic route is as follows.

To a stirred solution of tert-butyl 5-amino-1H-indole-1-carboxylate (1, 5.0 g, 21.55 mmol) in acetonitrile (50 mL) at 0 C., N-bromosuccinimide (4.23 g, 23.70 mmol) was added portion-wise. The mixture was stirred at same temperature for 3 h. Next, the reaction was poured into ice-cold water and extracted with ethyl acetate. The organic layer was washed with brine solution, dried over anhydrous sodium sulfate, filtered, and concentrated to dryness under reduced pressure. The crude product was purified by Combiflash (40 g, RediSep column) using 0-30% ethyl acetate in hexanes as eluent. The desired fractions were concentrated under reduced pressure to afford tert-butyl 5-amino-4-bromo-1H-indole-1-carboxylate (2) as a brown liquid. Yield: 5.8 g, 86%; MS (ESI) m/z 311.08 [M+1]+., 166104-20-7

166104-20-7 1-Boc-5-Aminoindole 11593831, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; eFFECTOR Therapeutics, Inc.; ERNST, Justin T.; REICH, Siegfried H.; SPRENGELER, Paul A.; XIANG, Alan X.; (41 pag.)US2019/119256; (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

166104-20-7, 1-Boc-5-Aminoindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 2-chioro-3-nitro-6-(trifluoromethyl)pyridine (1.0 g, 4.4 rnmoi)and tert-hulyl 5-amino-1H-indoie-1-carboxylate (0.59 g, 4.4 mmol) in DMF (20 mL) was heated at 100 ¡ãC for 3 h. 4-Fluorobenzaldehyde (0.60 g. 4.9 mmol) was added to the mixture and the reaction was stirred for 30 mm followed by addition of sodium dithionite (2.3g. 13.2 rnrnol). After 12 h at100 ¡ãC the reaction was cooled, diluted with EtOAc (100 mnL), and washed with F120 (50 mL x 3). The organic layer was dried (Na2504), and concentrated in vacuo. Purification (FCC. 5i02, EtOAc/hexanes) afforded the title compound (1.1 g, 50percent). MS ESI): mass caicd. for C76H20F4N407, 496.1; mn/z found, 497.0 [M?++{it., 166104-20-7

As the paragraph descriping shows that 166104-20-7 is playing an increasingly important role.

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; BERRY, Cynthia G.B.; CHEN, Gang; JOURDAN, Fabrice Loic; LEBOLD, Terry Patrick; LIN, David Wei; PENA PINON, Miguel Angel; RAVULA, Suchitra; SAVALL, Bradley M.; SWANSON, Devin M.; WU, Dongpei; ZHANG, Wei; AMERIKS, Michael K.; (407 pag.)WO2016/176460; (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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.166104-20-7,1-Boc-5-Aminoindole,as a common compound, the synthetic route is as follows.

To a solution of 2-bromo-3-((4-fluorophenyl)ethynyi)-6-methoxypyridine (1ntermediate 44, 531mg. 0867 mmol) in anhydrous toluene (9 rnL) was added XPhos (83 mg, 0.17 mmol), Pd2(dba)3(79 trig, 0088 mrnol), and potassium tert-butoxide (292 mg, 260 mmol). After 10 mimi. tert-butyi5-amino-i H-indole- I -carhoxylate (Intermediate ii, 201 trig. 0.867 mmnol) was added. The resultingsolution was refiuxed at 100 O(? for 3hr, then allowed to cool to 20 ¡ãC. The reaction was partitioned between EtOAc and water. The organic phase was separated, dried (MgSO4), filtered, and concentrated in vacuo, no deprotection necessary. Purification (FCC, Si02, 0percent to 30percent EtOAc/ heptanes) afforded the title compound (60 mg, 19percent) as a yellow solid. MS (ESI): mass caicd. forC22H,6FNO, 357.1; m/z found, 358 [M+Hr. ?H NMR (300 MHz, DMSO.-d6) oe 11.36 (s, iH, 7.53?7.42 (m, 3H), 7.41 ? 7.30 (m, 3H), 7.11 (t, J= 8.8 Hz, 2H), 6.92 (d, J= 8.5 Hz, 1H?), 6.85 (s, 1H?), 6.57 (d, J= 8.8 Hz, IH), 6.47 (s, IH), 3.90 (s, 3H)., 166104-20-7

The synthetic route of 166104-20-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; BERRY, Cynthia G.B.; CHEN, Gang; JOURDAN, Fabrice Loic; LEBOLD, Terry Patrick; LIN, David Wei; PENA PINON, Miguel Angel; RAVULA, Suchitra; SAVALL, Bradley M.; SWANSON, Devin M.; WU, Dongpei; ZHANG, Wei; AMERIKS, Michael K.; (407 pag.)WO2016/176460; (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