Zobrazeno 1 - 10
of 42
pro vyhledávání: '"Roger P. Bakale"'
Autor:
Joseph A. Sclafani, Jian Chen, Mina Gadelrab Dimitri, Mark A. Olsen, Christopher J. Neville, Christie Michael, Roger P. Bakale, Daniel V. Levy, Harlan F. Reese, Partha S. Mudipalli
Publikováno v:
Organic Process Research & Development. 21:1616-1624
TV-45070 is a small-molecule lactam containing a chiral spiro-ether that has been reported as a potential topical therapy for pain associated with the Nav1.7 sodium ion channel encoded by the gene SCN9A. A pilot-scale synthesis is presented that is h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::785c102845a287db1b21ebe1e121d7c5
https://doi.org/10.1021/acs.oprd.7b00237
https://doi.org/10.1021/acs.oprd.7b00237
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ec21e0c7f9669dcf7d81e1a7566b1156
https://doi.org/10.1021/acs.oprd.7b00070
https://doi.org/10.1021/acs.oprd.7b00070
An Improved Synthesis of the Free Base and Diglycolate Salt of CEP-33779; A Janus Kinase 2 Inhibitor
Publikováno v:
Organic Process Research & Development. 20:2085-2091
CEP-33779 is a triazole that has been reported to show highly selective inhibition of Janus kinase 2 (JAK2). An efficient process to form CEP-33779 will be presented that uses multiple palladium couplings to provide the drug substance in a convergent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7f1da7df622155b420ae3f6bed23776c
https://doi.org/10.1021/acs.oprd.6b00311
https://doi.org/10.1021/acs.oprd.6b00311
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9ae56591f1fc2c09acd4501f446347e8
https://doi.org/10.1002/ejoc.201500906
https://doi.org/10.1002/ejoc.201500906
Publikováno v:
Organic Process Research & Development. 18:1427-1433
In the development of a new route to bendamustine hydrochloride, the API in Treanda, the key benzimidazole intermediate 5 was generated via catalytic heterogeneous hydrogenation of an aromatic nitro compound using a batch reactor. Because of safety c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bf918b33bbe09c6281ffaf2c0fa4cb19
https://doi.org/10.1021/op400179f
https://doi.org/10.1021/op400179f
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afac1d5536d5d3fe35a2e1b5f3aa666d
https://doi.org/10.1021/ol400432x
https://doi.org/10.1021/ol400432x
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::177273f36058c730df872197d022d1ac
https://doi.org/10.1021/op300233g
https://doi.org/10.1021/op300233g
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00935fd5414acce5bb9fd2a65eaeabea
https://doi.org/10.1021/ol203332j
https://doi.org/10.1021/ol203332j
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...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::87652bb6c8d2133a00f6705e1d407d35
https://doi.org/10.1021/op200313v
https://doi.org/10.1021/op200313v
Autor:
Daniel V. Levy, Henry J. Breslin, Joseph A. Sclafani, Bruce D. Dorsey, Gregory R. Ott, Tho V. Thieu, Roger P. Bakale, Andrew McLean
Publikováno v:
Organic Letters. 13:4204-4207
The synthesis of a new kinase inhibitor template 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazine is described which includes a late stage orthogonally reactive key intermediate amenable to rapid diversification as well an optimized in situ triflate di
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::113264902338733b336ff27c9adf2d53
https://doi.org/10.1021/ol2015237
https://doi.org/10.1021/ol2015237