Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Michael A. Staszak"'
Autor:
Bruce W. Shaw, Yuke Zhang, Kenneth C. Cassidy, Robert M. Christie, Prabhakar Kondaji Jadhav, Jim D. Durbin, Gary G. Deng, Matthew Allen Schiffler, Kostas Gavardinas, Richard A. Brier, Keyun Qing, Donald P. Matthews, Michael A. Staszak, William F. Matter, Yong Wang, Kim Euibong Jemes, D. Scott Coffey
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1138-1142
Cathepsin S (Cat S) plays an important role in many pathological conditions, including abdominal aortic aneurysm (AAA). Inhibition of Cat S may provide a new treatment for AAA. To date, several classes of Cat S inhibitors have been reported, many of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6393a9fc5f96e20e55b6bf40e534a7b3
https://doi.org/10.1021/ml500283g
https://doi.org/10.1021/ml500283g
Autor:
Amy C. DeBaillie, Michael A. Staszak, Michael E. Laurila, Nicholas A. Magnus, Chauncey D. Jones
Publikováno v:
Organic Process Research & Development. 17:231-238
An efficient and scalable process for the preparation of a purine-based CB2 agonist was developed. The production route to the requisite purine core relies on N-acylation and sequential substitution of a 5-amino-4,6-dichloropyrimidine with two amine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6f7e95e2c4bdb6a095149312fed45fd7
https://doi.org/10.1021/op300278c
https://doi.org/10.1021/op300278c
Autor:
Christopher W. Doecke, Michael J. Martinelli, Pawlak Joseph Matthew, D. Scott Coffey, Richard D. Miller, Timothy M. Braden, Jeffrey Thomas Vicenzi, Steven Wayne Pedersen, Bruce W. Shaw, Michael E. LeTourneau, Christopher L. Meyer, Schmid Christopher Randall, and Michael A. Staszak
Publikováno v:
Organic Process Research & Development. 11:431-440
The first kilogram-scale synthesis of the PPARα agonist LY518674 (1) is described. The de novo convergent synthetic approach involved coupling of two rapidly assembled components, triazolone formation via a novel acid-promoted cyclization reaction,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0dd9fd5b6d28e178e92176fe99739e5a
https://doi.org/10.1021/op700040v
https://doi.org/10.1021/op700040v
Autor:
Bruce W. Shaw, Michael A. Staszak, Michael E. Laurila, Nicholas A. Magnus, Peter B. Anzeveno, D. Scott Coffey, David A. Hay, Jeffrey M. Schkeryantz
Publikováno v:
Organic Process Research & Development. 11:560-567
An asymmetric enantioselective aryl transfer reaction was developed to give access to the diarylmethanol 7 and ultimately acetate 2 which is useful for the preparation of mGlu2 receptor potentiators (Scheme 3). The aryl transfer chemistry involved th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d7ad172b985c31bd4583ee9dcaca9a14
https://doi.org/10.1021/op0602268
https://doi.org/10.1021/op0602268
Autor:
Michael J. Martinelli, Christa D. Sturgill, Chaoyu Xie, Michael A. Staszak, Vien V. Khau, Quatroche John Thomas
Publikováno v:
Organic Process Research & Development. 9:730-737
Nucleosidic phosphoramidites are key building blocks for the automated, solid supported syntheses of oligonucleotide-based drugs. A safe, industrially viable process for preparing nucleosidic phosphoramidites 5-Me-MOE-U and MOE-A has been developed a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::db110ec53f92bec554bbfede54dd996b
https://doi.org/10.1021/op050077d
https://doi.org/10.1021/op050077d
Autor:
Michael E. LeTourneau, Gregory A. Stephenson, Bruce E. Parker, Lisa M. H. Zollars, Jason S. Cronin, Nicholas A. Magnus, James Abraham Aikins, John P. Schafer, Susan M. Reutzel-Edens, and Shella L. Tameze, Michael A. Staszak, Amy D. Hargis, William D. Diseroad
Publikováno v:
Organic Process Research & Development. 9:621-628
This article describes the development and optimization of chemical reactions and subsequent preparation of the API LY503430 under cGMPs to fund first human dose (FHD) clinical evaluation as a potential therapeutic agent for Parkinson's disease. Reas
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d221a6e2a65d84e6e8be32a0a3d52af0
https://doi.org/10.1021/op0500741
https://doi.org/10.1021/op0500741
Publikováno v:
Organic Process Research & Development. 8:670-673
4-Methoxyphenylbutyric acid (2) is smoothly demethylated in 3 h at 180 °C when melted with pyridinium hydrochloride (Pyr·HCl), affording 4-hydroxyphenylbutyric acid (3), a key starting material for the preclinical candidate LY518674 (1). The adapta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6d744140b2f2d1c4707b55603160c0d4
https://doi.org/10.1021/op0499526
https://doi.org/10.1021/op0499526
Autor:
Michael E. Kopach, John L. Grutsch, Uko E. Udodong, Margaret M. Faul, Jeffrey Thomas Vicenzi, Michael A. Staszak, Christine A. Krumrich, Kevin A. Sullivan, Kobierski Michael Edward
Publikováno v:
Tetrahedron. 59:7215-7229
N-(Azacycloalkyl)bisindolylmaleimides 1 have been identified to be selective inhibitors of PKCβ. This manuscript will describe the synthetic approaches employed to prepare this class of compounds that resulted in development of efficient methods for
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3754422089b9a9f7ff1ead1b08e2e36a
https://doi.org/10.1016/s0040-4020(03)00973-6
https://doi.org/10.1016/s0040-4020(03)00973-6
Autor:
Gazak Robert James, Jerry W. Misner, Matt R. Reinhard, Gardner John Paul, Fisher Jack Wayne, Kristina L. Trinkle, Jeffrey Thomas Vicenzi, John R. Rizzo, Eugene Paul Kroeff, Eugene Farkas, James Abraham Aikins, Steve W Pedersen, Michael A. Staszak, Billy G. Jackson, Chris A Higginbotham, Christopher W. Doecke, Tony Y. Zhang
Publikováno v:
Tetrahedron. 56:5667-5677
Serine hydroxymethyltransferase (SHMT) derived from recombinant E. coli was found to be able to catalyze the condensation between glycine and 4-pentenaldehyde, affording enantiopure l -erythro-2-amino-3-hydroxy-6-heptenoic acid (AHHA) in high yield a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::835560431d5b61f966a3c79c24446498
https://doi.org/10.1016/s0040-4020(00)00416-6
https://doi.org/10.1016/s0040-4020(00)00416-6
Publikováno v:
Organic Process Research & Development. 13:1199-1201
The N-methylation of electron-deficient pyrroles was affected using dimethyl carbonate in the presence of DMF and catalytic DABCO. This alkylation methodology has proven useful for the alkylation o...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::85f18d28de1129e88d51a44ee45429a1
https://doi.org/10.1021/op900256t
https://doi.org/10.1021/op900256t