Action des composes organomagnesiens sur les pyrones-2-VII
作者:P. Lhoste、M. Moreau、J. Dreux
DOI:10.1016/s0040-4020(01)91804-6
日期:1984.1
In the reaction between organomagnesiumcompounds and 2-pyrones, the relative stability of the 6-hydroxy 5,6-dihydro 2H-pyrans and their tautomeric forms (ketols) has no influence on the reaction pathway. When ethylenic ketols are obtained, the corresponding tautomeric dihydropyranols are prepared in a selective way by reaction of nucleophilic reagents on the 3,6-dihydro-2-pyrones. In the other hand
The present invention provide a lubricating oil composition suitable for internal combustion engines, which composition is excellent in thermal/oxidation stability and can inhibit the increases of the viscosity and acid number even in the presence of NOx and can be used for a long period of time or provide a lubricating oil composition particularly suitable for diesel or direct injection engines equipped with an exhaust-gas after-treatment device such as DPF or various catalysts, which composition is excellent in high-temperature detergency and base number retention properties and further can achieve the effect of inhibit wear caused by soot contamination in the oil occurring significantly when the content of phosphorus compounds such as ZnDTP is decreased, at a high level and can inhibit the exhaust-gas after-treatment device from being adversely affected. The lubricating oil composition comprises a lubricating base oil containing, a specific amount of a base oil with specific properties, and two or more types of additives selected from specific additives.
CBI DERIVATIVES SUBJECT TO REDUCTIVE ACTIVATION
申请人:Boger Dale
公开号:US20110112163A1
公开(公告)日:2011-05-12
A unique class of N-acyl O-amino phenol prodrugs of CBI-TMI and CBI-indole
2
were synthesized and shown to be prodrugs, subject to reductive activation by nucleophilic cleavage of a weak N—O bond, effectively releasing the free drug in functional cellular assays for cytotoxic activity approaching or matching the activity of the free drug, yet remain essentially stable to ex vivo DNA alkylation conditions. Most impressively, assessment of the in vivo antitumor activity of a representative O-(acylamino) prodrug, 8, indicate that they approach the potency and exceed the efficacy of the free drug itself (CBI-indole
2
), indicating that the inactive prodrugs not only effectively release the free drug in vivo, but that they offer additional advantages related to a controlled or targeted release in vivo.