Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Todd S. Mcdermott"'
Publikováno v:
Powder Technology. 212:240-252
The aim of this study was to develop a material-sparing method to quantitatively measure sticking during tablet manufacturing and to allow direct comparison of blends in terms of sticking. A protocol has been developed for quantitation of API layerin
Autor:
Michael J. Rozema, Albert W. Kruger, Lakshmi Bhagavatula, Kenneth M. Engstrom, Thomas B. Borchardt, Jorge Gandarilla, Todd S. McDermott, Brian J. Kotecki, Ahmad Y. Sheikh, Steven J. Wittenberger, Seble Wagaw
Publikováno v:
Organic Process Research & Development. 13:1145-1155
A convergent, scalable synthesis of dipeptidyl peptidase-4 inhibitor, ABT-279, has been developed and demonstrated on multikilogram scale. The cis-2,5-disubstituted pyrrolidine is generated by cyclization of a Boc-amine onto an alkynyl ketone followe
Autor:
Michael G. Fickes, Zhenping Tian, Shyamal Parekh, Todd S. Mcdermott, Sou-Jen Chang, Steven J. Wittenberger, Ashok K. Gupta, Dilinie P. Fernando, David R. Hill
Publikováno v:
Organic Process Research & Development. 6:329-335
A process for the preparation of matrix metalloproteinase inhibitor ABT-518 has been developed. Significant improvements have been made to the first generation synthesis and are described here. The new process is very robust and efficient; multikilog
Publikováno v:
The Journal of Organic Chemistry. 63:2715-2718
Publikováno v:
ChemInform. 29
Autor:
Todd S. McDermott, T. Howard Black
Publikováno v:
Synthetic Communications. 20:2959-2964
4,4-Dialkyl 3,3-dichloro oxetan-2-ones rearrange under Lewis acid catalysis, accompanied by loss of HC1, to afford 4,5-dialkyl 3-chloro butenolides. We have recently been investigating the reactions of beta lactones under the influence of Lewis acid
Publikováno v:
Tetrahedron. 46:2307-2316
Cyclic and acyclic ketones were converted in three steps into 3-alkenoic acids, bearing a variety of substituents in the α -position. The sequence, involving ionization/elimination of a β-lactone, affords high yields of pure products uncontaminated
Publikováno v:
Tetrahedron Letters. 31:6617-6620
4-Cyclohexyl 3,3-disubstituted oxetan-2-ones rearrange under Lewis acid catalysis to afford trans-fused cycloheptano butyrolactones.
Autor:
Todd S. McDermott, Maureen A. McLaughlin, Michael J. Rozema, Bridget D. Rohde, Michael G. Fickes
Publikováno v:
ChemInform. 38
The stereoselective synthesis of A-345665.0 1, a novel farnesyl transferase inhibitor, is described. The key step involves a stereoselective addition of an imidazolyl Grignard reagent to aldehyde 8 in the presence of an external chiral auxiliary. Cry
Autor:
Daisy Pireh, Hana Kopecka, David W A Beno, James S. Polakowski, Kent D. Stewart, Thomas H. Lubben, James M. Trevillyan, Glenn A. Reinhart, Anita J Kempf-Grote, Richards Steven J, Lakshmi Bhagavatula, Jason A. Segreti, Michael A. Stashko, Paul E. Wiedeman, David Madar, Kenton L. Longenecker, Hing L. Sham, Steven J. Wittenberger, Xiaofeng Li, Heidi Wells, Thomas W. von Geldern, Ryan M. Fryer, Zhonghua Pei, Bradley A. Zinker, Michelle A. Long, Michael G. Fickes, Amanda K Mika, Todd S. Mcdermott, Stevan W. Djuric, Stephen J. Ballaron, Hong Yong
Publikováno v:
Journal of medicinal chemistry. 49(21)
Dipeptidyl peptidase-IV (DPP-IV) inhibitors are poised to be the next major drug class for the treatment of type 2 diabetes. Structure-activity studies of substitutions at the C5 position of the 2-cyanopyrrolidide warhead led to the discovery of pote