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The TMSOTf mediated nucleophilic cleavage of α-aminoacetals can be used to prepare a variety of substituted amines, with variable levels of stereocontrol depending on the substitution patterns. The reaction most likely proceeds via either an α-alkoxy aziridinium ion or an α-oxocarbenium ion depending on the type of nucleophile.
The development of a sensitive radioimmunoassay (RIA) for the determination of the potential anti-migraine drug GR151004 in human plasma is described. The validated method was used for the determination of the drug in plasma samples collected during a Phase I safety tolerability study in healthy volunteers. Synthetic routes for the hapten and radioligand are presented. Immunogen synthesis was performed...
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