Pyrrolidone derivatives

Although there is no evidence that the neuronal degeneration of AzD results, as in cardiovascular ischaemia, from the excitotoxicity of increased intracellular Ca +, some calcium channel blockers have been tried in AzD. They have had little effect but surprisingly a pyrrolidone derivative nefiracetam, which opens L-type voltage-sensitive calcium channels (VSCCs) reduces both scopolamine- and )S-amyloid-induced impairments of learning and memory in rats (Yamada et al. 1999). This effect can be overcome by VSCC antagonists, but nefiracetam has not been tried in humans. 

Lawesson s reagent converts pyrrolidone derivatives into thioxopyrrolidones, and peptides into thioxopeptides. ... 

Scheme 2.135. Synthesis of complex tricyclic pyrrolidone derivatives.

The interactions between the components that make up a photopolymer are extremely important in arriving at a working formulation. Here we show that inclusion of pyrrolidone derivatives like NVP or NMP in acrylate systems enhances the ambient cure of a film. From the reactivity parameters of some simple systems we have derived an empirical scheme for the formulation of fully and/or partially reactive systems based on the molar equivalent ratios of the acrylate to pyrrolidone components. The data support the presence of a synergistic effect between NVP and the acrylate components. 

Lactam-Benzoin Initiator Interaction. We have shown that whenever one of these pyrrolidone derivatives is present, the ambient cure is enhanced. A variety of reasons can be responsible, including the ones proposed above, however a possibility not discussed is the interaction between an excited state of the photoinitiator and the lactam. Spectroscopic data showed no changes in the DMPA absorption spectrum with addition of NVP. 

Pyrrolidine and pyrrolidone derivatives with phosphorus-containing substituents 93MI1. 

Other methods for preparing 3-alkyl- and 3,3-di-alkyl-2-pyrrolidone derivatives of the current investigation are described (3). 

The use of Cremophore EL in the microemulsions is avoided nowadays due to several adverse effects such as anaphylactic shocks and histamine release [20 ]. The other important consideration is the concentration of surfactants and co-surfactants which should be minimal and preferably not exceed 20%. Furthermore, it is necessary to ensure that the microemulsion structure is preserved in the presence of the tonicity adjusting solutions such as 0.9% saline solution and preservatives. The parenteral microemulsions should also be able to withstand tests such as freeze-thaw cycling which ensure their physical stability. It has been shown that the colloidal carriers based on Solutol HS 15 can withstand freeze-thaw cycling very efficiently whereas lecithins can offer stability to autoclaving [ 112 ]. Cosurfactants such as benzyl alcohol cannot be used for intravenous applications but can be used for the small volume parenteral products up to the concentration of 1% w/v. Ethanol at concentrations above 10% usually results in the pain on injection. Co-surfactants such as glycofurol are reported to acceptable for parenteral products but there are no products based on glycofurol available for the human use. The pyrrolidone derivatives are reported to be acceptable for veterinary applications. 

None of the substances caused significant enzyme secretion by macrophages. Only the pyrrolidone derivative (3a) caused a slight increase of LDH with increasing dose of the polymer. This finding corresponds to the higher acute toxicity of (3b) as compared to unsubstituted DIVEMA derivative (1b). 

Syntheses and biological evaluation of (+ )-lactacystin (2-pyrrolidone derivative, a secondary metabolite from Streptomyces) and analogs 00EJO2513. 

An interesting subsequent reaction has been observed for a series of 1,1 -dial ky 1- 3 - but e ny 1 phenyl ketones the resulting unsaturated carboxamides cyclize to pyrrolidone derivatives ... 

Butanediol is used entirely as a precursor for other intermediates, polymers, and solvents. Its principal derivatives are tetrahydrofuran, butyrolac-tone, and pyrrolidones. Tetrahydrofuran can be polymerized to polytetra-methylene ether glycol (PTMEG), a key component in manufacturing spandex fibers. Another derivative, 7-butyrolactone, is a solvent used primarily for spinning polyester fibers. Pyrrolidones such as normal methyl pyrrolidone (NMP) are used as extraction solvents for producing lubricating oils. Other pyrrolidone derivatives are used as binders for pharmaceuticals. 

S-(-)-levetiracetam is a pyrrolidone derivative unrelated to the structures of other AEDs. It is indicated as an adjunct in the treatment of partial onset seizures in adults, and It has shown some benefit In clinical trials for generalized tonic-clonic seizures (GTC) and myoclonic seizures in adults and children (79,80). 

SW 751 (21) the pyrrolidone derivative R 40244 (32). However, no details are known about the primary mode of action of these herbicides dichlormate and pyrichlor most likely interfere directly with carotene formation... 

Sasaki, H., Kojima, M., Nakamura, J., and Shibasaki, J. (1990a). Acute toxicity and skin irritation of pyrrolidone derivatives as transdermal penetration enhancer, Chem. Pharm. Bull, 38 2308-2310. 

In the chapter on olefinic reactions, it was observed that mild hydrogenation of MA produces succinic anhydride (SA). Further reduction of SA can give rise to y-butyrolactone 102. This can be accomplished catalytically on a platinum catalyst.y-Butyrolactone 102 can also be further reduced to THF 103. Both these products are commercially significant. In 1976, 83 MM lb of THF were produced in the United States.Most of this is derived from acetylene as raw material. y-Butyrolactone 102 is also a good solvent, intermediate, and monomer, and can be converted to pyrrolidone derivatives. 

Ring contraction. Startg. m. refluxed 3 hrs. under Ng with NaH in glyme, then acidified with anhydrous oxalic acid pyrrolidone deriv. Y 87%. K. Yamada et al., Am. Soc. 94, 8278 (1972). 

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