Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Shawn P. Allwein"'
Publikováno v:
Organic Process Research & Development. 22:1236-1240
Spiro[1H-pyrido[2,3-d][1,3]oxazine-4,4′-piperidine]-2-one (3) is a key building block in many biologically active compounds. The synthesis of this compound, as reported in the literature, is low-yielding. We have discovered and developed a robust,
Autor:
Christie Michael, James J. Reif, Dale R. Mowrey, Karen L. Milkiewicz, Roger P. Bakale, Mark A. Olsen, Vikram C. Purohit, Shawn P. Allwein, Christopher J. Neville, Gregory J. Gilmartin, Daniel E. Petrillo
Publikováno v:
Organic Process Research & Development. 21:740-747
The development of a scalable route to TEV-37440, a dual inhibitor of focal adhesion kinase (FAK) and anaplastic lymphoma kinase (ALK), is presented. The medicinal chemistry route used to support this target through nomination is reviewed, along with
Autor:
Shawn P. Allwein, Christopher J. Neville, Christie Michael, Karen L. Milkiewicz, Mildred L. Kaufman, Daniel V. Levy, Yi Wang, Nelson G. Landmesser, Linli He, Mark A. Olsen, Kannan Muthukumaran
Publikováno v:
Organic Process Research & Development. 21:408-413
Cinchona alkaloid-based thiourea catalysts (1a and 1b) belong to an important class of bifunctional organocatalysts, which has been widely used for a variety of asymmetric reactions. The commercial availability of these catalysts is sporadic, and lim
Publikováno v:
CORROSION. 72:1292-1299
During routine pharmaceutical development and scale-up work, severe corrosion of a Hastelloy Alloy C-22 (Alloy 22) filter dryer was observed after single, short (several hour) contact with the product slurry at room temperature. Initial investigation
Autor:
Linli He, Melanie Marguerit, Roger P. Bakale, Shawn P. Allwein, Jason Rossi, James J. Reif, Yi Wang, Renee C. Roemmele, Gill Little
Publikováno v:
European Journal of Organic Chemistry. 2015:8003-8010
A total synthesis of enantiomerically pure [14C]-labelled (–)-homoharringtonine in 17 steps is reported. This synthetic process enabled the production of Good Manufacturing Practice (GMP) compliant (–)-[14C]homoharringtonine that was used in a hu
Publikováno v:
Organic Letters. 15:1650-1653
An efficient, catalytic hypervalent iodine-mediated oxidative 1,2-shift of 1,1'-disubstituted olefins is described. This methodology provides concise access to homobenzylic ketones with electron-donating substituents. In the case of cyclic systems, t
Publikováno v:
Organic Process Research & Development. 16:1861-1865
A cost-effective one-pot synthesis of Fmoc-O-benzylphospho-l-serine, an amino acid commonly used in the synthesis of phosphorylated peptides, has been developed. Two methods for executing this synthesis are described, and both have been scaled to pro
Publikováno v:
Organic Letters. 14:1206-1209
Fmoc-O-benzyl-l-phosphoserine is an important building block in the synthesis of Forigerimod, a phosphopeptide being investigated for Systemic Lupus Erythematosus (SLE). An efficient one-pot process was developed using inexpensive, readily available
Autor:
Shawn P. Allwein, Dale R. Mowrey, Renee C. Roemmele, Diane E. Gingrich, Roger P. Bakale, Daniel E. Petrillo, James J. Haley, James J. Reif
Publikováno v:
Organic Process Research & Development. 16:148-155
Evolution of the process strategies to prepare CEP-28122, an anaplastic lymphoma kinase (ALK) inhibitor, is presented. The initial medicinal chemistry route, used for the preparation of key supplie...