33602-03-8Relevant academic research and scientific papers
Oxidation of N-acyl-pyrrolidines to imides with CrO3·3,5- dimethylpyrazole
Blay, Gonzalo,Cardona, Luz,Garcia, Begona,Garcia, Cristina L.,Pedro, Jose R.
, p. 8257 - 8260 (2007/10/03)
N-Acyl-pyrrolidones are easily obtained by treatment of N-acyl- pyrrolidines with CrO33,5-dimethylpyrazole complex (CrO33,5-DMP) at room temperature.
Synthesis and anticonvulsant activity of 1-acyl-2-pyrrolidinone derivatives
Sasaki,Mori,Nakamura,Shibasaki
, p. 628 - 633 (2007/10/02)
Several 1-acyl-2-pyrrolidinone derivatives were synthesized as derivatives of γ-aminobutyric acid (GABA), and their pharmacological activities and stabilities were investigated. The derivatives showed anticonvulsant effect on picrotoxin-induced seizure at a dose of 200 mg/kg. In particular, 1-decanoyl-2-pyrrolidinone (7) and 1-dodecanoyl-2-pyrrolidinone (8) had a high activity. The anticonvulsant activity showed a dose dependency. Some of 1-acyl-2-pyrrolidinone derivatives prolonged sleeping time which was induced by sodium pentobarbital and showed a recovery from disruption of the memory of passive avoidance response, which was induced by an electroconvulsive shock. As shown by the results of the stability study of 1-acetyl-2-pyrrolidinone (1), it was degraded in an acidic buffer and an alkaline buffer although 2-pyrrolidinone was stable. 1-Acyl-2-pyrrolidinone derivatives were degraded in liver and brain homogenates of mouse and rat. They showed a degradation rate in rat plasma. Conversion of 8 to GABA in mouse liver homogenate was demonstrated. These results suggested that the pharmacological activity of 1-acyl-2-pyrrolidinone is probably due to the release of GABA by hydrolysis of derivatives although further work is necessary.
