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Dive into the research topics where Gregory P. Roth is active.

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Featured researches published by Gregory P. Roth.


Tetrahedron Letters | 1991

Catalyst tailoring for palladium-mediated cross coupling of arylstannanes with vinyl triflates

Vittorio Farina; Gregory P. Roth

Abstract Vinyl triflates couple smoothly with a variety of arylstannanes provided a polar, aprotic solvent is used in conjunction with a “ligandless” palladium catalyst, or catalytic system involving weak ligands such as triphenylarsine. Commonly employed ligands, for example, triphenylphosphine, were found to strongly inhibit the coupling.


Bioorganic & Medicinal Chemistry Letters | 2008

Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3

Martin E. Hayes; Grier A. Wallace; Pintipa Grongsaard; Agnieszka Bischoff; Dawn M. George; Wenyan Miao; Michael J. McPherson; Robert H. Stoffel; David W. Green; Gregory P. Roth

High-throughput screening identified a low molecular weight antagonist of CXCR3 displaying micromolar activity in a membrane filtration-binding assay. Systematic modification of the benzimidazole core and tethered acetophenone moiety established tractable SAR of analogs with improved physicochemical properties and sub-micromolar activity across both human and murine receptors.


Bioorganic & Medicinal Chemistry Letters | 1994

Taxol® structure-activity relationships: synthesis and biological evaluation of taxol analogs modified at C-7

Shu-Hui Chen; Joydeep Kant; Stephen W. Mamber; Gregory P. Roth; Jianmei Wei; Daniel R. Marshall; Dolatrai M. Vyas; Vittorio Farina; Annamaria Casazza; Byron H. Long; William C. Rose; Kathy A. Johnston; Craig R. Fairchild

Abstract A series of taxol derivatives, modified at C-7, is described. This includes sulfonate, silylether, ester, carbonate, carbamate, fluoro, dehydro and deoxy derivatives. Biological evaluation shows that these modifications do not usually significantly compromise activity. However, none of the C-7 analogs prepared thus far have been shown to be better than taxol in both in vitro and in vivo assays.


Tetrahedron Letters | 1993

Trimethylsilylfluorosulfonate (TMSOFs): An alternative to TMS triflate as a source of Me3Si+

Bruce H. Lipshutz; Jana Burgess-Henry; Gregory P. Roth

Abstract Generation of trimethylsilylfluorosulfonate in situ provides a useful source of TMS+, the reactivity of which in essentially equivalent to that of TMS triflate. Its precursors, in particular FSO3H, are less costly than those of TMSOTf or the reagent itself


Tetrahedron Letters | 1991

Palladium in cephalosporin chemistry: an inexpensive triflate replacement for palladium acetate mediated coupling reactions

Gregory P. Roth; Chester Sapino

Abstract 3-Fluorosulfonyloxy-3-cephems are easily prepared and subsequent palladium(0) catalyzed coupling with various vinylstannanes proceeds in excellent yields with stereospecific transfer of the alkene fragment.


Tetrahedron Letters | 1992

Alkoxycarbonylation Reactions Using Aryl Fluorosulfonates

Gregory P. Roth; Jeanine Thomas

Abstract Aryl fluorosulfonates are shown to undergo palladium catalysed alkoxycarbonylation with a variety of alcohols under mild basic conditions at ambient CO pressure.


Synthetic Communications | 1990

Palladium in Cephalosporin Chemistry: Mild Triflate Couplings in the Absence of Phosphines and Halide Donors

Stephen R. Baker; Gregory P. Roth; Chester Sapino

Abstract Palladium catalyzed triflate-organostannane couplings are shown to proceed in a very mild manner in the absence of added phosphine and halide reagents. This protocol has been demonstrated for 3-trifloxycephems and vinyl triflates.


Bioorganic & Medicinal Chemistry Letters | 2008

Lead identification of 2-iminobenzimidazole antagonists of the chemokine receptor CXCR3.

Martin E. Hayes; Eric C. Breinlinger; Grier A. Wallace; Pintipa Grongsaard; Wenyan Miao; Michael J. McPherson; Robert H. Stoffel; David W. Green; Gregory P. Roth

Modification of a 2-iminobenzimidazole series derived from an HTS hit resulted in compounds with improved in-vitro species selectivity. Incorporation of an 8-quinoline amide and conformational rigidification of an aliphatic tether furnished potent compounds suitable for further lead optimization.


Tetrahedron Letters | 1995

Reaction of paclitaxel and 10-desacetyl baccatin III with diethylamino sulfurtrifluoride

Gregory P. Roth; Daniel R. Marshall; Shu-Hui Chen

Abstract Reaction of protected paclitaxel with diethylamino sulfurtrifluoride (DAST), to furnish the 7-fluoro paclitaxel, gives a mixture of four products, two of which have not been previously reported. The product distribution is shown to be solvent dependent. An efficient process for the preparation of the parent 7-α-fluoro baccatin III from 10-desacetyl baccatin III is also described.


Tetrahedron Letters | 1995

An interesting c-ring contraction in paclitaxel (Taxol®)

Shu-Hui Chen; Stella Huang; Gregory P. Roth

Abstract An interesting pinacol rearrangement involving 7-epi-6α-tosylate/triflate-paclitaxel derivatives ( 6 ) and ( 10 ), with the formation of five-membered C-ring containing analogs ( 7 ) and ( 11 ), is described.

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Shu-Hui Chen

Florida State University

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Kevin P. Cusack

Rensselaer Polytechnic Institute

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