123546-85-0Relevant academic research and scientific papers
Diastereoselective access to trans -2-substituted cyclopentylamines
Joosten, Antoine,Lambert, Emilie,Vasse, Jean-Luc,Szymoniak, Jan
supporting information; experimental part, p. 5128 - 5131 (2011/01/05)
A highly diastereoselective synthesis of trans-2-substituted cyclopentylamines via a tandem hydrozirconation/Lewis acid-mediated cyclization sequence applied to butenyl oxazolidines is described. The method allows an easy preparation of diversely substituted cyclopentylamines which appear to be useful synthetic intermediates. This was further illustrated by the syntheses of (±)-Rodocaine, (±)-trans-pentacin, and enantiomerically enriched trans-cyclopentane-1,2-diamine.
Disubstituted tetrahydrofurans and dioxolanes as PAF antagonists
Bartroli,Carceller,Merlos,Garcia-Rafanell,Forn
, p. 373 - 386 (2007/10/02)
A new series of disubstituted tetrahydrofuran and dioxolane derivatives were prepared and evaluated for their PAF antagonist activity in the PAF-induced in vitro platelet-aggregation and in vivo hypotension tests. Several of these compounds exhibited more potent activity than the structurally related 2-[N-acetyl-N-[[[[2-methoxy-3-[(octadecylcarbamoyl)oxy]propoxy] carbonyl]amino]methyl]-1-ethylpyridinium chloride (CV-6209, 3) in the in vitro assay, whereas all showed less potency in the in vivo test. The role of both the substituent nature and the placement and number of oxygen atoms in the ring are discussed. A qualitative SAR study was carried out on these nuclei.
