[Objective] An objective of the present invention is to provide compounds that are effective against various resistant bacteria which cause current clinical problems, for example, pneumococci including penicillin resistant
Streptococcus pneumoneae
(PRSP),
Haemophilus influenzae
including bata-lactamase-nonproducing ampicillin-resistant
Haemophilus influenzae
(BLNAR), and
Moraxella
(
Branhamella
)
catarrhalis.
[Structure] The present invention provides 2-ethenylthio-based carbapenem derivatives represented by the formula (I) or pharmaceutically acceptable salts thereof that are effective, for example, against pneumococci including penicillin resistant
Streptococcus
pneumoneae (PRSP),
Haemophilus influenzae
including beta-lactamase-nonproducing ampicillin-resistant
Haemophilus influenzae
(BLNAR), and
Moraxella
(Branhamella) catarrhalis:
Forty-seven tert. amines were examined in order to observe the relative lability of the various N-substituents in respect to cleavage by ClCO2Et in refluxing benzene. The aromatic amines did not react with ClCO2Et, while aliphatic and alicyclic amines were cleaved to give carbamate (s) ; the tendency to cause R-N cleavage was : benzyl>allyl>methyl>ethyl>other alkyl groups. It was found that the reaction of a tert. amine with ClCO2Et is greatly influenced by the polarity of the solvent, reaction temperature and N-substituents.
BMIm HCO<sub>3</sub>: an ionic liquid with carboxylating properties. Synthesis of carbamate esters from amines
作者:A. Di Nicola、A. Arcadi、L. Rossi
DOI:10.1039/c6nj02705a
日期:——
1-Butyl-3-methylimidazolium hydrogen carbonate (BMIm HCO3) was used as an ionic liquid with carboxylating properties able to convert, in the presence of an alkyl halide, amines into the corresponding carbamate esters. Moderate to good yields of carbamates were obtained according to the nature of the amine and the alkylating agent.
This invention relates to a range of alpha substituted 2-benzyl substituted imidazole compounds and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.