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Disclosed are a fused pyrimidine derivative o f formula (I), and a pharmaceutically acceptable salt, stereoisomer, hydrate and solvate thereof, which have an excellent inhibitory activity on FMS kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating diseases caused by abnormal activation o f FMS kinases such as immunologic diseases, metabolic diseases, inflammatory diseases, cancers and tumors.

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Reference:
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

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Unexpected regioselectivity for the Skraup-Doebner-Von Miller reaction was observed during the synthesis of quinolines from 4-aminoindoles and acetone in the presence of hydrochloric acid as a catalyst. The products were unambiguously assigned as 1-alkyl-3,5,5-trimethyl-5,6-dihydro-1H-azepino[4,3,2-cd]indoles instead of 2,2,4-trimethyl-2,7-dihydro-1H-pyrrolo[2,3-h]quinolones based on NMR spectroscopy and X-ray crystallographic analysis.

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Reference:
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

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NOVEL CATIONIC 4-AMINOINDOLES, DYE COMPOSITION COMPRISING A CATIONIC 4-AMINOINDOLE, PROCESSES THEREFOR AND USES THEREOF

The present invention relates to a cationic4-aminoindole of general formula (I), addition salts thereof with an acid and solvates thereof: in which: R1 is a linear or branched, saturated C2-C20 alkyl radical, substituted and/or interrupted with a cationic radical. The present invention is also directed towards a process for synthesizing this cationic 4-aminoindole, to the compositions, the uses, the hair dyeing processes and the devices using this cationic 4-aminoindole.

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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

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The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 4769-97-5 is helpful to your research. Safety of 4-Nitroindole

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4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in?vitro and in?vivo

A series of 4,5-indolyl-N-hydroxyphenylacrylamides, as HDAC inhibitors, has been synthesized and evaluated in?vitro and in?vivo. 4-Indolyl compounds 13 and 17 functions as potent inhibitors of HDAC1 (IC50 1.28?nM and 1.34?nM) and HDAC 2 (IC50 0.90 and 0.53?nM). N-Hydroxy-3-{4-[2-(1H-indol-4-yl)-ethylsulfamoyl]-phenyl}-acrylamide (13) inhibited the human cancer cell growth of PC3, A549, MDA-MB-231 and AsPC-1 with a GI50 of 0.14, 0.25, 0.32, and 0.24?muM, respectively. In in?vivo evaluations bearing prostate PC3 xenografts nude mice model, compound 13 suppressed tumor growth with a tumor growth inhibition (TGI) of 62.2%. Immunohistochemistry of protein expressions, in PC-3 xenograft model indicated elevated acetyl-histone 3 and prominently inhibited HDAC2 protein expressions. Therefore, compound 13 could be a suitable lead for further investigation and the development of selective HDAC 2 inhibitors as potent anti-cancer compounds.

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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

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Cloning and expression of naphthalene dioxygenase genes from Comamonas sp. MQ for indigoids production

The naphthalene dioxygenase (NDO) genes were cloned from Comamonas sp. MQ and successfully expressed in Escherichia coli BL21 (DE3) (designated as ND-IND). The whole cells of recombinant strain ND-IND possessed relatively high transformation efficiency towards indole and most indole derivatives. According to the UV-vis and HPLC-MS analyses, the major products derived from the indoles could be indigo with different substituent groups. Furthermore, strain ND-IND was able to produce 205 mg/l indigo from 300 mg/l indole with a specific production rate of 8.4 mg/(g dry cell weight h). The effects of phenol, pyridine and quinoline on indigo production were determined, which indicated that phenol and pyridine had little inhibition on indigo production while quinoline would result in a 32% decrease in indigo yield. The present study proposed the potential application of recombinant strain ND-IND in indigoid pigments production, and offered the promise of applying strain ND-IND for the production of indigo using indole-containing wastewater as the raw materials.

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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

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Palladium acetate assisted synthesis of five-membered N-polyheterocycles

The metal-assisted synthesis of heterocyclic compounds is known to be one of the extremely developing as well as significant concepts of organic chemistry. Because of their expensive, complex working of the instrument and difficult procedures, the methodologies used earlier for the heterocycle synthesis were less amicable to the researchers. The Pd(OAc)2-mediated cyclic reactions have been recognized to be very effective for both the stereoselective as well as regioselective formation of the 5-membered N-bearing heterocyclic compounds. The different uses of palladium acetate, as a catalyst in the formation of 5-membered N-containing polyheterocycles, are covered in this review article.

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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

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Activation Relay on Rhodium-Catalyzed C-H Aminomethylation in Cooperation with Photoredox Catalysis

A site selective C-H aminomethylation at indole’s C3 position has been achieved by merging rhodium(III)-catalyzed C-H activation and photoredox catalysis in a one-pot manner. An investigation of the mechanistic insights rationalized the essence of the activation relay and the combination mode.

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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

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JNK modulators

Compounds of formula I modulate JNK: wherein the variables are as defined herein.

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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

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CONSTRUCTION OF OPTICALLY PURE TRYPTOPHANS FROM SERINE DERIVED AZIRIDINE-2-CARBOXYLATES

The possibility of preparing optically pure tryptophan derivatives from various substituted indoles and (2R)- or (2S)-2-aziridinecarboxylates has been examined.Zinc triflate was found to be the only Lewis acid capable of bringing about this reaction in moderate yields.

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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

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4769-97-5, 4-Nitroindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step A. 4-Nitro-1.3-dihvdro-2H-indol-2-oneA mixture of 4-nitroindole (12.2 g, 75.2 mmol) and N-chlorosuccinimide (6.07 g, 30.1 mmol) in CHCl3 (500 mL) was heated at reflux for 30 h, then concentrated under reduced pressure to give an orange solid. The solid was dissolved in AcOH (200 mL) and the resulting solution was warmed to 70 ¡ãC, then 85percent H3PO4 (80 mL) was added over 2 min. The mixture was heated to reflux for 90 min then cooled on ice. The cooled mixture was adjusted to pH 6 by addition of 10 N NaOH (450 mL), followed by aqueous NaHCO3, keeping the temperature below 30 ¡ãC. The mixture was extracted with EtOAc (3 x 1 L) and the combined organic extracts were dried over Na2SO4, filtered, and concentrated in vacuo. The crude product was partially purified by silica gel chromatography, eluting with a gradient of hexane: EtOAc – 100:0 to 0:100, and then triturated with MeOH to give the title compound. MS: m/z = 179 (M + 1).

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Reference£º
Patent; MERCK & CO., INC.; WO2008/153852; (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