54943-19-0

Upstream product

• 21892-80-8 3-methylbenzo[d]oxazol-2(3H)-one 
• 802294-64-0 propionic acid 
• 123-62-6 propionic acid anhydride 
• 54903-11-6 6-propanoyl-3H-1,3-benzoxazol-2-one 
• 74-87-3 methylene chloride 
• 33388-19-1 3-propionylbenzo[d]oxazol-2(3H)-one 
• 59-49-4 2-Benzoxazolinone 

Downstream Products

• 54903-58-1 1-(3-Hydroxy-4-methylamino-phenyl)-propan-1-one 
• 131363-44-5 3-methyl-6-{3-[4-(3-trifluoromethylphenyl)-1-piperazinyl]-2-methylpropionyl}benzoxazolinone 
• 131363-46-7 3-methyl-6-{3-[4-(2-methoxyphenyl)-1-piperazinyl]-2-methylpropionyl}benzoxazolinone 
• 134577-30-3 2,4-Dimethyl-7-propionyl-4H-benzo[1,4]oxazin-3-one 
• 134577-33-6 7-(2-methylenepropionyl)-2,4-dimethyl-3,4-dihydro-3-oxo-1,4(2H)benzoxazine 
• 134577-34-7 7-(2-methylenepropionyl)-2,2,4-trimethyl-3,4-dihydro-3-oxo-1,4(2H)benzoxazine 

Relevant academic research and scientific papers

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.

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.