Výsledky vyhledávání - "V. John Jasys"

Process Development of CP-481715, a Novel CCR1 Antagonist

Autor: Kathleen S. Zandi, William Kissel, Brian M. Andresen, Chiu Charles K, John Charles Kath, David C. Whritenour, Matthew Frank Brown, Tung Le, Z. Jane Li, Eric Dias, Richard A. Buzon, Michel Couturier, Bryan Li, John L. Tucker, V. John Jasys, Joanna Teresa Negri, Poss Christopher Stanley, Frank J. Urban

Publikováno v: Organic Process Research & Development. 9:466-471

Process development for the synthesis of 2-quinoxalinecarboxamide, N-[(1S,2S,4R)-4-(aminocarbonyl)-1-[(3-fluorophenyl)methyl]-2,7-dihydroxy-7-methyloctyl] is described. An optimized and streamlined process starting from lactone 2 was developed: Lacto

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2bfdf67bd0fea0a89f37efcd9381a33b
https://doi.org/10.1021/op050059w

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Streamlined Processes for the Synthesis of a Farnesyl Transferase Inhibitor Drug Candidate

Autor: Enrique Vazquez, Susan Deborah Lagreca, Mark Guinn, Michel Couturier, Marcus Ewing, Karl Ng, A. Morgan Stewart, Lulin Wei, Raggon Jeffrey W, Brian M. Andresen, John L. Tucker, V. John Jasys, Frank J. Urban, Garrett Moraski, Derek L. Tickner, Joel M. Hawkins, B. J. Cronin, Joseph Peter Lyssikatos, Michael D'occhio

Publikováno v: Organic Process Research & Development. 8:643-650

As part of a fast-paced oncology program, quinolinone 1 was discovered and developed as a potent inhibitor of farnesyl transferase for the treatment of cancer. The initial synthesis, which suffered from a lengthy linear sequence and a late-stage chro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::62f35f47fd9303eb09dc350ab597f78f
https://doi.org/10.1021/op049935g

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Process Research on [(2S)-(3-Fluorophenyl)-(1S)-(5-oxotetrahydrofuran- 2-yl)ethyl]carbamic Acid tert-Butyl Ester, a Lactone Intermediate for an Aspartyl Protease Inhibitor

Autor: Frank J. Urban, V. John Jasys

Publikováno v: Organic Process Research & Development. 8:169-175

Two processes for the preparation of lactone [2S-(3-fluorophenyl)-1S-(5-oxotetrahydrofuran-2-yl)ethyl]carbamic acid tert-butyl ester 1 starting from S-BOC-(3-fluorophenyl)alanine 3 are described. (S)-(3-Fluorophenyl)alanine N-methyl-N-methoxy amide 1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a9b5e9c4010c83a9b8deb760b0350d75
https://doi.org/10.1021/op030207n

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Novel Synthesis of 1-(1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)-3-[4-(1-hydroxy-1-methyl-ethyl)-furan-2-sulfonyl]urea, an Anti-inflammatory Agent

Autor: John D. Weaver, Richard A. Buzon, Raggon Jeffrey W, James F. Eggler, Paul D. Hill, V. John Jasys, Frank J. Urban

Publikováno v: Synthetic Communications. 33:2029-2043

A novel synthesis of the anti-inflammatory agent 1-(1,2,3,5,6,7- hexahydro-s-indacen-4-yl)-3-[4-(1-hydroxy-1-methyl-ethyl)-furan-2-sulfonyl] urea 1 is described. Sulfonamide 5 was prepared starting from ethyl 3-furoate 2. Key steps were a one-pot sul

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90b35460ac9fada93ff99a5abe82176a
https://doi.org/10.1081/scc-120021029

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Preparation of Fluoroadamantane Acids and Amines: Impact of Bridgehead Fluorine Substitution on the Solution- and Solid-State Properties of Functionalized Adamantanes

Autor: Robert A. Volkmann, Appleton Troy A, V. John Jasys, and Martine Ziliox, Franco Lombardo, Jon Bordner

Publikováno v: Journal of the American Chemical Society. 122:466-473

Functionalized adamantanes are utilized as medicinal therapeutics and a practical route to novel bridgehead fluorinated adamantylamines and acids including fully fluorinated 3,5,7-tri-fluoroadamantane-1-carboxylic acid 1 and 3,5,7-trifluoroadamantane

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::80fad89c03c8b37d1d2d1e764d037ded
https://doi.org/10.1021/ja992652x

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Inhibition of human leukocyte elastase (HLE) by novel bicyclic β-lactams

Autor: Rebecca Williams, Robert A. Volkmann, Alice V. Bakker, Robin W. Spencer, W. Stephen Faraci, V. John Jasys, Michael S. Kellogg

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 3:2271-2276

Novel 3,2,0 bicyclic β-lactam sulfenamides and selected carbon isosteres are inhibitors of human leukocyte elastase. The comparative biological activity and hydrolytic stability of these compounds are described.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e8f6cb453dbd3fbb0648cd980fc0bd4a
https://doi.org/10.1016/s0960-894x(01)80938-0

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Observation of a new dimeric amino acid derivative in the reaction of methyl N-BOC-(S)-(3-fluorophenyl)alanate with DIBAL-H and lithio ethyl propiolate

Autor: V. John Jasys, Frank J. Urban

Publikováno v: Tetrahedron: Asymmetry. 12:361-363

A novel amino acid dimer 9a was isolated while trying to apply a known reduction/nucleophilic addition sequence. This dimer provided information both on the mechanism of the process and on the dependence of the desired reaction on the stoichiometry o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b772e39d8b98309e7503c8365586389c
https://doi.org/10.1016/s0957-4166(01)00054-4

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Novel quaternary ammonium salt-containing polyamines from the Agelenopsis aperta funnel-web spider

Autor: Paul R. Kelbaugh, Kenneth J. Rosnack, James T. Forman, Robert A. Volkmann, Nicholas A. Saccomano, V. John Jasys, Deane M. Nason, Phillips Douglas, Justin G. Stroh

Publikováno v: The Journal of Organic Chemistry. 57:1814-1820

Two novel hydroxylamine-containing acylpolyamines, Agel 489a and Agel 505a, each bearing a terminal quaternary ammonium salt, were isolated from the venom of Agelenopsis aperta, a funnel-web spider found throughout the western United States. Publishe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::51e80b227014be2e920ea85f5a8e921f
https://doi.org/10.1021/jo00032a039

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Synthesis of novel sulfenamide-containing β-Lactams

Autor: Michael S. Kellogg, Robert A. Volkmann, V. John Jasys

Publikováno v: Tetrahedron Letters. 32:3771-3774

Novel sulfenamide-containing [3,2,0]bicyclic β-lactams, which are potent inhibitors of human leukocyte elastase, were prepared.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6cbd12aab498c6f156f7d5224b012483
https://doi.org/10.1016/s0040-4039(00)79372-5

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The total synthesis of argiotoxins 636, 659 and 673

Autor: Paul R. Kelbaugh, Nicholas A. Saccomano, Robert A. Volkmann, V. John Jasys, Deane M. Nason, Phillips Douglas

Publikováno v: Tetrahedron Letters. 29:6223-6226

Practical syntheses of three polyamine spider toxins isolated from the venom of Argiope aurantia are described.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::07c8650adecab7b40e36d7b68c7c5519
https://doi.org/10.1016/s0040-4039(00)82310-2

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