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Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analogues.
Salvinorin A is the most potent naturally occurring opioid agonist yet discovered with high selectivity and affinity for kappa-opioid receptor. To explore its structure and activity relationships, aExpand
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8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents
A novel series of fully synthetic 8-azatetracyclines was prepared and evaluated for antibacterial activity. Compounds were identified that overcome both efflux (tet(K)) and ribosomal protectionExpand
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Process R&D of Eravacycline: The First Fully Synthetic Fluorocycline in Clinical Development
Process research and development of the first fully synthetic broad spectrum 7-fluorotetracycline in clinical development is described. The process utilizes two key intermediates in a convergentExpand
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Recent advances in aryl C-glycoside synthesis.
Aryl C-glycosides are stable analogs of the corresponding O-glycosides. Because of their favorable pharmacological profiles attributed primarily to the C-glycosyl moiety, aryl C-glycosides haveExpand
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Highly Enantioselective Syntheses of Functionalized α-Methylene-γ-butyrolactones via Rh(I)-catalyzed Intramolecular Alder Ene Reaction: Application to Formal Synthesis of (+)-Pilocarpine
A highly enantioselective Rh(I)-catalyzed intramolecular Alder ene reaction has been developed. The desired products, 3-vinyl, vinyl acetate, and vinyl ether-substitued α-methylene-γ-butyrolactonesExpand
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Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy.
Utilizing a fully synthetic route to tetracycline analogues, the C-9 side-chain of the fluorocyclines was optimized for both antibacterial activity and oral efficacy. Compounds were identified thatExpand
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Highly enantioselective cycloisomerization of enynes catalyzed by rhodium for the preparation of functionalized lactams.
The rising demand for chiral raw materials, intermediates, and active ingredients in pharmaceuticals, agrochemicals, food additives, and fragrances provides the impetus for rapid developments inExpand
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Highly enantioselective Rh-catalyzed intramolecular Alder-ene reactions for the syntheses of chiral tetrahydrofurans.
Alder±ene reactions are a powerful way to construct carbon±carbon bonds. The intramolecular version of these reactions can provide efficient routes to produce a variety of heterocyclic andExpand
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Rh-catalyzed kinetic resolution of enynes and highly enantioselective formation of 4-alkenyl-2,3-disubstituted tetrahydrofurans.
Rh-catalyzed cycloisomerization of enynes ether with a substituent at the allylic position was examined using (rac)-BINAP, and excellent selectivity was observed. When enantiomerically pure BINAP wasExpand
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Synthesis and in vitro pharmacological studies of new C(4)-modified salvinorin A analogues.
Salvinorin A, a compound isolated from the plant Salvia divinorum, is a potent and highly selective agonist for the kappa opioid receptor. For exploration of its structure and activity relationships,Expand
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