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Poly (ethylene glycol)-bound sulphonic acid as a novel catalyst for synthesis of benzoxazoles

ABSTRACT Ahighly efficient, simple and rapid method for the preparation of various 2-aminobenzoxazoles and other benzoxazole derivatives using a catalytic amount of poly (ethylene glycol)-bound sulphonic acid (PEG-SO3H) is described. PEG-SO3H is found to be economical and reusable catalyst with low catalytic loading. The percentage yield was found to be satisfactory, experimental set-up and purification of final products is facile and easy. GRAPHICAL ABSTRACT.

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A selective synthesis of the fullerene-fused dioxane adduct via heterogeneous reaction of C60 with alpha-diols and NaOH under ultrasonication

A novel ultrasonic-mediated approach to the synthesis of 1,9-dihydro[C60-Ih][5,6](1,4-dioxano)fullerene based on the heterogeneous reaction of fullerene with alpha-diols and NaOH has been developed. It allows producing the fullerene derivatives with high yields and selectivity.

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Synthesis of 2-aminobenzoxazoles using tetramethyl orthocarbonate or 1,1-dichlorodiphenoxymethane

The synthesis of 2-aminobenzoxazoles can be readily achieved by two versatile, one-pot procedures utilizing commercially available tetramethyl orthocarbonate or 1,1-dichlorodiphenoxymethane, an amine, and an optionally substituted 2-aminophenol. The reactions were conducted under mild conditions and provided 2-aminobenzoxazoles in modest to excellent yields. A variety of amines and substituted 2-aminophenols were used to investigate the scope of the reactions.

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Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Review, the author is Flick, Andrew C. and a compound is mentioned, 4570-41-6, Benzo[d]oxazol-2-amine, introducing its new discovery. 4570-41-6

Synthetic Approaches to the New Drugs Approved during 2017

New drugs introduced to the market every year represent privileged structures for particular biological targets. These new chemical entities (NCEs) provide insight into molecular recognition while serving as leads for designing future new drugs. This annual review describes the most likely process-scale synthetic approaches to 31 new chemical entities approved for the first time globally in 2017.

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Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.4570-41-6, you can also check out more blogs about4570-41-6

4570-41-6, In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 4570-41-6, name is Benzo[d]oxazol-2-amine, introducing its new discovery.

NOVEL HISTONE DEACETYLASE INHIBITORS

The present invention is a compound of the formula or a pharmaceutically acceptable salt thereof. The compounds are useful as HDAC inhibitors.

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A new NBS/oxone promoted one pot cascade synthesis of 2-aminobenzimidazoles/2-aminobenzoxazoles: A facile approach

A new strategy for the synthesis of 2-aminobenzimidazoles via a reaction of alpha-halogenated cyclohexanone with guanidine is reported. It provides a facile N-bromosuccinimide (NBS) mediated transition metal free, sustainable path for the synthesis of 2-substituted azoles. NBS along with the oxone promotes in situ halogenation of cyclohexanone, which in turn, when allowed to react with guanidine, afforded 2-aminobenzimidazoles (2-ABI). This eco-friendly protocol provides a competent laboratory synthesis method associated with significant advantages such as greater selectivity, cost-efficiency, mild reaction conditions, absence of chromatographic purification, clean reaction profile, and a simple work-up procedure to furnish high yields. The structures of all the synthesized compounds were confirmed on the basis of IR, 1H and 13C NMR, mass spectrometry, and elemental analyses data. In addition, we have also extended the scope of this strategy for obtaining 2-amino substituted benzoxazoles.

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.4570-41-6, Name is Benzo[d]oxazol-2-amine, molecular formula is C7H6N2O, 4570-41-6. In a Article, authors is Stec, Markian M.£¬once mentioned of 4570-41-6

Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: Investigations of various 6,5-heterocycles to improve metabolic stability

N-(6-(6-Chloro-5-(4-fluorophenylsulfonamido)pyridin-3-yl)benzo[d] thiazol-2-yl)acetamide (1) is a potent and efficacious inhibitor of PI3Kalpha and mTOR in vitro and in vivo. However, in hepatocyte and in vivo metabolism studies, 1 was found to undergo deacetylation on the 2-amino substituent of the benzothiazole. As an approach to reduce or eliminate this metabolic deacetylation, a variety of 6,5-heterocyclic analogues were examined as an alternative to the benzothiazole ring. Imidazopyridazine 10 was found to have similar in vitro potency and in vivo efficacy relative to 1, while only minimal amounts of the corresponding deacetylated metabolite of 10 were observed in hepatocytes.

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IMIDAZOLE-CONTAINING INHIBITORS OF ALK2 KINASE

Disclosed are compounds of formula (I), (II), (III), and (IV), and pharmaceutically acceptable salts thereof. The compounds are inhibitors of ALK2 kinase. Also provided are pharmaceutical compositions comprising a compound of formula (I), (II), (III), or (IV), or pharmaceutically acceptable salt thereof, and methods involving use of the compounds or pharmaceutically acceptable salts thereof and compositions in the treatment and prevention of various diseases and conditions, such as fibrodysplasia ossificans progressiva.

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Access to Amide from Aldimine via Aerobic Oxidative Carbene Catalysis and LiCl as Cooperative Lewis Acid

Herein, an efficient route to amides from aldimines via aza-Breslow intermediates through aerobic oxidative carbene catalysis with LiCl as a cooperative Lewis acid is described. Many of the obtained N-heteroarylamides feature biological activity. Ambient air was used as the sole oxidant and source of oxygen in this catalytically oxidative amidation. This method allows for a broad substrate scope and mild conditions. The aza-Breslow intermediate derivative was isolated and its crystal structure confirmed.

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Synthesis of 5H-Benzoxazolo<3,2-a>quinazolin-5-ones

5H-Benzoxazolo<3,2-a>quinazolin-5-ones (Xa-d) were synthesized in excellent yields from N-(2-hydroxyphenyl)anthranilic acids (Ia-d) and cyanogen bromide.The synthesis was based on the mechanistic consideration of the reactions of salicylic acid with cyanogen bromide previously reported in the literature.A versatile alternative route to these novel heterocyclic compounds was through thermal cyclization of N-(2-benzoxazolyl)-2-fluorobenzamides (XIII) obtained by reacting 2-fluorobenzoyl chloride with 2-aminobenzoxazoles.The reaction of Xb with ethanol in the presence of potassium hydroxide gave an ethoxyquinazolinone (XVII).Similarly, the alkaline hydrolysis of Xb afforded an quinazolindione (XVIII).

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Benzoxazole – Wikipedia,
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