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Artemisinin and a Series of Novel Endoperoxide Antimalarials Exert Early Effects on Digestive Vacuole Morphology
The synthesis of a novel series of epoxy-endoperoxides that can be prepared in high yields from simple starting materials are reported on and suggest that the digestive vacuole is an important initial site of endoperoxide antimalarial activity. Expand
Novel endoperoxide antimalarials: synthesis, heme binding, and antimalarial activity.
A series of novel epoxy endoperoxide compounds that can be prepared in high yields in one to three steps from simple starting materials are reported, suggesting that some of the endoperoxides may exert their antimalarial activities by a novel mechanism of action. Expand
Discovery of BNC375, a Potent, Selective, and Orally Available Type I Positive Allosteric Modulator of α7 nAChRs.
A novel class of compounds with either Type I or Type II behavior that can be tuned by the relative stereochemistry around the central cyclopropyl ring is reported, led to the discovery of BNC375, a small molecule with good CNS-drug like properties and clinical candidate potential. Expand
Concise, stereoselective syntheses of cis-nemorensic acid and 4-hydroxy-cis-nemorensic acid via tandem carbonyl ylide formation-cycloaddition.
[reaction: see text] 1,3-Dipolar cycloaddition of propargyl bromide with the carbonyl ylide derived from 6-diazoheptane-2,5-dione is the key step in concise syntheses of cis-nemorensic acid andExpand
1,2-dioxines containing tethered hydroxyl functionality as convenient precursors for pyran syntheses.
A new method for the construction of tetrahydropyrans derived from readily available 1,2-dioxines containing a tethered hydroxyl moiety is described. The reaction proceeds via a base-catalyzedExpand
First examples of the catalytic asymmetric ring-opening of meso 1,2-dioxines utilising cobalt(II) complexes with optically active tetradentate Schiff base ligands: formation of enantio-enriched
The combination of chiral cobalt beta-ketoiminato or cobalt salen complexes and meso 1,2-dioxines leads to catalytic asymmetric ring-opening affording enantio-enriched cis gamma-hydroxy enones;Expand
Stereocontrolled syntheses of the nemorensic acids using 6-diazoheptane-2,5-dione in carbonyl ylide cycloadditions.
Subsequent oxidative cleavage of the ring originally derived from the cyclic carbonyl ylide intermediate provides a straightforward access to polysubstituted tetrahydrofurans, and in particular an efficient entry to the nemorensic acids. Expand
Mechanistic investigations on the reaction between 1,2-dioxines and bulky stabilized phosphorus ylides: an efficient route to closely related cyclopropane stereoisomers.
Enolate quenching of the intermediate 1-2lambda(5)-oxaphospholanes 4 prior to collapse results in an equilibrium mixture of intermediates 10 and 11 which have been fully characterized, and their formation is primarily a result of the steric bulk of the stabilized ester ylide. Expand
Synthesis and chemistry of 2,3-dioxabicyclo[2.2.2]octane-5,6-diols.
During the study of the chemistry of 2,3-dioxabicyclo[ 2.2.2]octane-5,6-diols a hitherto unknown rearrangement was discovered which has wide applicability for the synthesis of 1,4-dicarbonyls, including optically enriched synthons. Expand
The first total synthesis of natural grenadamide.
A concise, high yielding route to the naturally occurring enantiomer of grenadamide utilizing a 3,6-disubstituted 1,2-dioxine starting material is presented. The route allows for ease in synthesizingExpand