Addition of the lithium derivatives of phosphine oxides Ph,P(O)CH,R' to aldehydes gives erythro adducts (1 1 ) with good stereoselectivity. Reduction of a-diphenylphosphinoyl ketones (I 2) gives threo adducts ("1 1 ) with even better stereoselectivity. Purification b y flash chromatography and/or crystallisation followed by elimination of Ph,PO,)gives pure Zor E-alkenes with high material conversion. Explanations are offered for the stereoselectivities, conditions defined for full stereochemical control, and guidelines suggested for approaches to a given alkene.
A series of N-substituted 3-aminoglutarimides have been synthesized and tested for inhibitory activity against a range of chemokines in vitro and for suppression of lipopolysaccharide-induced inflammation in vivo. The results show that they represent the first class of small molecules with broad-spectrum chemokine inhibitory effects. Among the compounds studied, 10 (NR58,4) was the most potent, being active at doses between 5 and 15 nM in vitro and at 0.3 mg kg(-1) in vivo.
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