A series of 4 00 -O-acyl derivatives of 8a-aza-8a-homoerythromycins A were synthesized and tested against Gram-positive and Gram-negative bacteria. Derivatives of 8a-aza-8a-homoerythromycin A have potent anti-bacterial activity against not only azithromycin-susceptible strains, but also efflux (M) and inducible macrolide-lincosamide-streptogramin-resistant Gram-positive pathogens. These compounds show moderate to high clearance and low oral bioavailability in preliminary in vivo pharmacokinetic studies in rat.
Selective oxidation of diethylene glycol by a ruthenium(VIII) species, obtained in situ from ruthenium(III) chloridesodium periodate in the presence of a catalytic quantity of water, affords a monoaldehyde in the form of the internal acetal 2-hydroxy-1,4-dioxane. This compound was used in reductive alkylations of selected primary and secondary amines, demonstrating its utility in the preparation of target structures with the 2-(2-hydroxyethoxy)ethylamino unit.
. -Title compound (I) is found to be a useful aldehyde for the reductive alkylation of amines to give (2-hydroxyethoxy)amines in varying yields. The hydroxydioxane itself is prepared by careful Ru-catalyzed monooxidation of diethylene glycol with sodium periodate and isolated as dichloromethane solution. -(VINTER*, A.; AVDAGIC, A.; STIMAC, V.; PALEJ, I.; CIKOS, A.; SUNJIC, V.; ALIHODZIC, S.; Synthesis 2010, 2, 255-258; GlaxoSmithKline Res.
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