54903-63-8

Upstream product

• 21892-80-8 3-methylbenzo[d]oxazol-2(3H)-one 
• 98-88-4 benzoyl chloride 
• 93-97-0 benzoic acid anhydride 
• 65-85-0 benzoic acid 
• 54903-12-7 6-benzoyl-2(3H)-benzoxazolone 
• 74-87-3 methylene chloride 
• 59-49-4 2-Benzoxazolinone 
• 13787-59-2 3-benzoyl-2(3H)-benzoxazolone 

Downstream Products

• 54903-59-2 (3-Hydroxy-4-methylamino-phenyl)-phenyl-methanone 
• 116337-62-3 7-Benzoyl-2,2,4-trimethyl-4H-benzo[1,4]oxazin-3-one 
• 116337-61-2 7-Benzoyl-4-methyl-4H-benzo[1,4]oxazin-3-one 
• 116363-84-9 7-Benzoyl-2,4-dimethyl-4H-benzo[1,4]oxazin-3-one 
• 848926-02-3 C₁₅H₁₃NO₃ 

Relevant academic research and scientific papers

FeCl3-DMF complex as efficient catalyst for the synthesis of 6-acyl-2(3H)-benzoxazolones and 6-acyl-2(3H)-benzothiazolones

FeCl3-DMF complex has been tested on Friedel-Crafts reaction of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone with acid chlorides and anhydrides as acylating agents. In these conditions, the 6-acyl-2(3H)-benzoxazolones and 6-acyl-2(3H)-benzothiazolones were obtained in yields ranging from 52 to 89%. Among the various commonly catalysts; AlCl3-DMF, ZnCl2-DMF and PPA, explored in this study, the best conditions using FeCl3-DMF were found the most convenient one

New imidazole derivatives of 2(3H)-benzazolones as potential antifungal agents

A series of new imidazole derivatives containing 2(3H)-benzoxazolone or 2(3H)-benzothiazolone ring were synthesized as analogues of the antifungal drug bifonazole. All compounds were tested in vitro against Candida albicans, Candida parapsilosis, and Cand

Aromatase inhibitor compounds and uses thereof

The invention concerns the use of a compound of formula (I) inhibitor of aromatase for the preparation of a pharmaceutical formulation intended for treatment of cancer or psoriasis. It equally relates to compounds of formula (I), notably for their use as active ingredients of a medication.

Unsymmetrical Diarylketones from Electron-rich Heterocyclic Arenes

AlCl3-mediated chlorocarbonylation of a first arene by oxalyl chloride followed by in situ Friedel-Crafts acylation of a second electron-rich arene expeditiously provides, in a one-pot procedure, either symmetrical or unsymmetrical benzophenones with yields ranging from 17-52%. Best results are obtained when the more activated substrate is used as the second arene. Another advantage is that the resultant benzophenone precipitates from the reaction mixture allowing facile workup.

Friedel-crafts acylation of 2(3H)-benzoxazolone: Investigation of the role of the catalyst and microwave activation

To study the scope and limitations of the use of complexed species of AlCl3 in Friedel-Crafts reactions, we investigated the acctylation and benzoylation of 2(3H)-benzoxazolone and 3-methyl-2(3H)-benzoxazolone varying the amide complexing agent. We replaced dimethylformamide by N-methylformamide, dimethylacetamide, pyrrolidone, N-methylpyrrolidone, tetramethylurea, and dimethylsulfoxide. However, there was no particular advantage of substituting dimethylformamide by another amide ligand. This can probably be ascribed to the fact that the complex formed between AlCl3 and the complexing agent becomes too stable. Alternatively, a route using polyphosphoric acid and microwave activation was explored. The major advantage of running the reaction in a microwave oven was that a good yield was reached in a rather short period of time.

Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)- benzothiazolone derivatives

A series of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives were synthesized and evaluated for anticonvulsant activity. The compounds were assayed, intraperitoneally in mice and per os in rats, against seizures induced by maximal electroshock (MES) and pentylene-tetrazole (scMet). Neurologic deficity was evaluated by the rotarod test. The compounds were prepared to determine the relationship between the 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives' structures and anticonvulsant activity. Several of these compounds showed significant anticonvulsant activity. Compounds 43 and 45 were the most active of the series against MES-induced seizures with ED50 values of 8.7 and 7.6 mg/kg, respectively. Compound 45 displayed good protection against MES-induced seizures and low toxicity in rats with an oral ED50 of 18.6 mg/kg and a protective index (PI = TD50/ED50) of 1 receptors with nanomolar affinities.

CATALYTIC ACYLATION OF BENZOXAZOLIN-3-ONES IN THE PRESENSCE OF ZINC CHLORIDE

In the acylation of benzoxazolin-2-ones by aromatic acid chlorides in the presence of 10-2 mole ZnCl2, the yields of the corresponding 6-aroylbenzoxazolin-2-ones depend on the electronegativity of the acylating agent and the nucleophilicity of

A Convenient and Efficient Method for the Preparation of 6-Acyl-2(3H)-benzoxazolones

Benzoxazolinone derivatives have been found to exhibit various pharmacological properties and 6-acyl-2(3H)-benzoxazolones are considered as key starting materials for the preparation of these compounds.Reported here are the optimal conditions for a regioselective acylation at the 6-position of the benzoxazolinone ring.A general method leading to the expected products in excellent yields consists in using a mixture of aluminum chloride-dimethylformamide as catalyst and acid anhydrides or chlorides as acylating agents.

Acyl-7 dihydro-2,3 benzoxazin-1,4 ones-3 et proprietes normolipemiantes

7-Acyl-2,3-dihydro-1,4-benzoxazin-3-ones and normolipemic properties.Fibrates are still among the most widely used drugs for the treatment of dyslipoproteinemia. 7-Acyl-2,3-dihydro-1,4-benzoxazin-3-ones (Fig.1B) can be considered as conformationally restrained analogues of fibrates, such as fenofibrate.These compounds have been prepared and studied for their normolipemic activity particularly on plasma cholesterol, triglyceride and high density lipoprotein (HDL) cholesterol levels.Hepatotoxicity and mutagenicity have also been evaluated.Some of them show an interesting activity, quite comparable to fenofibrate, and are devoid of hepatotoxicity. hyperlipidemia / hypocholesterolemic drugs / fibrates / 7-acyl-1,4-benzoxazin-3-ones