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Rapid access to enantiopure bupropion and its major metabolite by stereospecific nucleophilic substitution on an α-ketotriflate
Abstract A stereospecific method for the synthesis of enantiopure α-aminoketone from its corresponding α-hydroxy-ketone via the triflate intermediate is discussed. This strategy provides a rapid andExpand
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A superior method for the reduction of secondary phosphine oxides.
[reaction: see text] Diisobutylaluminum hydride (DIBAL-H) and triisobutylaluminum have been found to be outstanding reductants for secondary phosphine oxides (SPOs). All classes of SPOs can beExpand
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An improved method of amide synthesis using acyl chlorides
A simple, mild and highly efficient condition for amide synthesis from acyl chlorides has been developed to minimize hydrolysis, racemization and other side reactions. This method should expandExpand
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Overcoming barriers to green chemistry in the pharmaceutical industry – the Green Aspiration Level™ concept
TLDR
We propose the Green Aspiration Level™ (GAL) concept as a novel process performance metric that quantifies the environmental impact of producing a specific pharmaceutical agent while taking into account the complexity of the ideal synthetic process for producing the target molecule. Expand
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Biological actions of formoterol isomers.
Racemic beta(2) agonists, composed of equal amounts of (R)- and (S)-isomers, can display anomalous actions that compromise their effectiveness as asthma therapies. Loss of efficacy during regular useExpand
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Activation of TMSCN by N-heterocyclic carbenes for facile cyanosilylation of carbonyl compounds.
N-Heterocyclic carbenes were found to be highly effective organocatalysts in activating TMSCN for facile cyanosilylation of carbonyl compounds. Cyano transfer from TMSCN to aldehydes and ketonesExpand
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Vibrational circular dichroism of amylose carbamate: structure and solvent-induced conformational changes
The conformational changes of amylose tris-(dimethylphenylcarbamate) (ADMPC) in the presence of polar solvents were investigated by VCD spectroscopy for the first time. The conformation of ADMPC wasExpand
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Chromatographic and spectroscopic studies on the chiral recognition of sulfated beta-cyclodextrin as chiral mobile phase additive enantiomeric separation of a chiral amine.
A fast enantiomeric separation of a chiral aromatic amine was achieved, using ultra high pressure liquid chromatography and highly sulfated beta-cyclodextrin (S-beta-CD) as a chiral additive in theExpand
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Efficient synthesis of Empagliflozin, an inhibitor of SGLT-2, utilizing an AlCl3-promoted silane reduction of a β-glycopyranoside.
An efficient production synthesis of the SGLT-2 inhibitor Empagliflozin (5) from acid 1 is described. The key tactical stage involves I/Mg exchange of aryl iodide 2 followed by addition to gluconoExpand
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