Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Gregory J. Withbroe"'
Autor:
Gerald A. Weisenburger, Brian Patrick Chekal, Janice E. Sieser, Brian C. Vanderplas, David B. Damon, Michael St. Pierre, John G. Van Alsten, Carlos Mojica, Kyle R. Leeman, Danny Lafrance, Carrie Wager, Shu Yu, Rajappa Vaidyanathan, Gregory J. Withbroe, Karen Sutherland, Andrew S. Palm
Publikováno v:
Organic Process Research & Development. 19:1944-1953
A de novo three-step-one-pot process for the formation of PF-04191834 was developed. This methodology employed inexpensive, odorless, and readily available commodity chemical iso-octyl-3-mercaptopropionate as a sulfur source, which could be a general
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b86ed2168e64162a477212d79c402d9c
https://doi.org/10.1021/op500412a
https://doi.org/10.1021/op500412a
Autor:
Ronald J. Post, Charles W. Palmer, Robert William Mclaughlin, Robert A. Singer, Brian Patrick Chekal, Janice E. Sieser, Gregory W. Sluggett, Rajappa Vaidyanathan, Steven M. Guinness, Gregory J. Withbroe, Brett M. Lillie
Publikováno v:
Organic Process Research & Development. 18:266-274
The manufacturing process of axitinib (1) involves two Pd-catalyzed coupling reactions, a Migita coupling and a Heck reaction. Optimization of both of these pivotal bond-formation steps is discussed as well as the approach to control impurities in ax
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f8f8f76600e2280574e1d32f6c2573eb
https://doi.org/10.1021/op400088k
https://doi.org/10.1021/op400088k
Autor:
Gregory J. Withbroe, Chris Seadeek, Rajappa Vaidyanathan, Brian C. Vanderplas, Kevin P. Girard, Steven M. Guinness
Publikováno v:
Organic Process Research & Development. 17:500-504
This article describes a systematic approach used to streamline the process for the isolation of bosutinib monohydrate, a promiscuous solvate former. A thorough understanding of the complex solid form landscape was garnered, and this knowledge was us
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7eb02567bcf10cd24f2de6af0d80d8f4
https://doi.org/10.1021/op300087r
https://doi.org/10.1021/op300087r
Publikováno v:
Organic Process Research & Development. 12:480-489
We describe the efficient preparation of Bippyphos, 1. The key precursor to Bippyphos, 5, was prepared via a one-pot bromination of diketone 2 followed by alkylation with pyrazole and condensation with phenylhydrazine. Lithiation of 5 and trapping wi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2ad80af0f966b40a1affc610f2946c46
https://doi.org/10.1021/op7002858
https://doi.org/10.1021/op7002858
Autor:
Chiara Bezze, Robert A. Singer, Megan McMahon, Mariano Stivanello, Gregory J. Withbroe, Handfield Robert Eugene, Paul E. Concannon, Jason D. McKinley, Timothy J. N. Watson, Lucia Leoni, Busch Frank R
Publikováno v:
Synthetic Communications. 38:441-447
Described here is the synthesis of (1‐(aminomethyl)‐2,3‐dihydro‐1H‐inden‐3‐yl)methanol 1, the previously unidentified impurity found in the synthesis of 2,1 providing a confirmation of the structure. Fabbrica Italiano Sintetici (FIS), w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a9dcf0aa90dba515a31c7601f9c2c138
https://doi.org/10.1080/00397910701771231
https://doi.org/10.1080/00397910701771231
Autor:
William H. Martin, Banavara L. Mylari, Peter J. Oates, James B. Coutcher, Michael C. Linhares, David A. Tess, Michael S. Dina, David A. Beebe, Gregory J. Withbroe, Sandra J Armento, Melissa O'Gorman, William James Zembrowski, Edward L. Conn
Publikováno v:
Journal of Medicinal Chemistry. 48:6326-6339
Discovery of a highly selective, potent, and safe non-carboxylic acid, non-hydantoin inhibitor of aldose reductase (AR) capable of potently blocking the excess glucose flux through the polyol pathway that prevails under diabetic conditions has been a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4950c5594f211c33eec4b7093b58b81
https://doi.org/10.1021/jm050462t
https://doi.org/10.1021/jm050462t
Publikováno v:
ChemInform. 39
We describe the efficient preparation of Bippyphos, 1. The key precursor to Bippyphos, 5, was prepared via a one-pot bromination of diketone 2 followed by alkylation with pyrazole and condensation with phenylhydrazine. Lithiation of 5 and trapping wi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::fbcd87545e7c8424052ff3eea4c2ffae
https://doi.org/10.1002/chin.200840045
https://doi.org/10.1002/chin.200840045
Autor:
David A. Beebe, James B. Coutcher, William James Zembrowski, Banavara L. Mylari, Peter J. Oates, Gregory J. Withbroe, Edward L. Conn, Nathaniel S. Brackett
Publikováno v:
Bioorganicmedicinal chemistry. 11(19)
Two new templates, (R) 2-hydroxyethyl-pyridine and (R) 2-hydroxyethyl-triazine, were used to design novel sorbitol dehydrogenase inhibitors (SDIs). The design concept included spawning of these templates to function as effective ligands to the cataly
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::362bad9374e7958ccde32d601b5ae785
https://pubmed.ncbi.nlm.nih.gov/12951149
https://pubmed.ncbi.nlm.nih.gov/12951149
Autor:
James B. Coutcher, Gregory J. Withbroe, Peter J. Oates, Melissa O'Gorman, Michael S. Dina, Edward L. Conn, William H. Martin, Banavara L. Mylari, William James Zembrowski, David A. Tess, David A. Beebe, Sandra J Armento, Michael C. Linhares
Publikováno v:
Journal of medicinal chemistry. 46(12)
We report here on the discovery path that led to a structurally unprecedented non-hydantoin, non-carboxylic acid aldose reductase inhibitor, 24, which shows remarkably potent oral activity in normalizing elevated sorbitol levels and, more significant
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::48a28c635fafc7155bc0c769f30e1bba
https://pubmed.ncbi.nlm.nih.gov/12773033
https://pubmed.ncbi.nlm.nih.gov/12773033
Autor:
Peter J. Oates, Michael C. Linhares, Gregory J. Withbroe, James B. Coutcher, Edward L. Conn, William James Zembrowski, Melissa O'Gorman, Banavara L. Mylari, David A. Beebe
Publikováno v:
Journal of medicinal chemistry. 45(20)
We report here a novel sorbitol dehydrogenase inhibitor, 16, that shows very high oral potency (50 microg/kg) in normalizing elevated fructose levels in the sciatic nerve of chronically diabetic rats and sustained duration of action (24 h). Furthermo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::09607f6a1fc5ec3ce9cd426c31c991df
https://pubmed.ncbi.nlm.nih.gov/12238919
https://pubmed.ncbi.nlm.nih.gov/12238919