Ring-chain tautomerism. Part 10 +. The reaction of oxocarboxylic acids with diazodiphenylmethane
The rate coefficients for the esterification of a series of oxocarboxylic acids with diazodiphenylmethane have been determined in ethanol or 2-methoxyethanol at 30.0°C. These and the rates of reaction with model compounds have been used to estimate the equilibrium constants for ring-chain tautomerism for the oxocarboxylic acids.
Bowden, Keith,Misic-Vukovic, Milica M.,Ranson, Richard J.
p. 1601 - 1606
(2007/10/03)
Prodrugs - Part 2. Acylbenzoate esters of metronidazole
The design and synthesis of a series of chain and cyclic acylbenzoate esters of metronidazole are described. The esters are designed to be both lipophilic and reactive in their hydrolysis reactions. The alkaline hydrolyses of the chain 2-acylbenzoates are relatively rapid, employing an intramolecular catalytic route, while the reactions of the 4-formylbenzoate and cyclic 2-formylbenzoate are also relatively rapid using the normal pathway. The anti-bacterial activity of the esters are comparable to that of metronidazole.
Bowden,Izadi
p. 995 - 1000
(2007/10/03)
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