Zobrazeno 1 - 10
of 24
pro vyhledávání: '"George T. Lee"'
Publikováno v:
Organic Process Research & Development. 14:883-889
A six-step synthesis of a 4-[8-(3-fluorophenyl)[1,7]naphthyridin-6-yl]-trans-cyclohexanecarboxylic acid with an overall yield of 27% starting from 2-cyano-3-methylpyridine, cyclohexane-1,4-dicarboxylic acid dimethyl ester, and 3-fluorophenylboronic a
Publikováno v:
Organic Process Research & Development. 12:1137-1141
An optimized convergent synthetic route for the preparation of retinoid X receptor (RXR) antagonist (1) in an overall yield of 35% is described. The formation of the benzodiazepine was achieved in 85% yield using POCl3 in toluene. The drug substance
Publikováno v:
Advanced Synthesis & Catalysis. 347:1921-1924
Coupling of different halogenated acetanilides with acrylates using Pd-catalyzed ortho-selective CH bond activation is reported. The yields of coupled products are low to high depending on the substrate. In general, arenes with electron-rich substitu
Publikováno v:
Journal of Heterocyclic Chemistry. 42:131-135
A general synthesis of 1,3-diaryl-4-pyrazoleacetic acid esters has been realized via the condensation of a γ-carboxy ester hydrazone with the Vilsmeier reagent.
Publikováno v:
Advanced Synthesis & Catalysis. 346:1461-1464
A facile highly regioselective process is described for the formation of 4-chloromethyl-1,3-oxazoles from 1,3-oxazole N-oxide/HCl salts. An explanation is presented for the high regioselectivity in deoxygenation-chlorination using POCl3 with HCl salt
Autor:
Wen-Chung Shieh, Robert Daeffler, Run-Ming Wang, Remo Gamboni, Song Xue, Friedrich Schuerch, Loeser Eric M, Gordon Florence and, Ian Paterson, Guang-Pei Chen, Daniel Niederer, Adnan Osmani, Frederick Ray Kinder, Kapa Prasad, Joseph Mckenna, Jacques Cercus, Klaus Schreiner, Gottfried Sedelmeier, Manuela Seger, Olivier Loiseleur, Kurt Königsberger, Timothy Michael Ramsey, Larry Rogers, Andrew Bach, Oljan Repic, Weichun Chen, Noela Reel, Dominique Bixel, Peng Geng, and Liladhar Waykole, and Karl Schaer, Stuart J. Mickel, Hans Stettler, George T. Lee
Publikováno v:
Organic Process Research & Development. 8:113-121
Coupling of C9-14 (4) and C15-21 (5a) fragments to produce the cis-trisubstituted olefin was achieved using Suzuki-type coupling conditions employed by Marshall (5a/tert-BuLi/B-OMe-9-BBN added to 4/Cs2CO3/Pd(dppf)2). The terminal (Z)-diene moiety was
Autor:
Stuart J. Mickel, Gottfried H. Sedelmeier, Daniel Niederer, Friedrich Schuerch, Guido Koch, E. Kuesters, Robert Daeffler, Adnan Osmani, Manuela Seeger-Weibel, E. Schmid, Alfred Hirni, Karl Schaer, Remo Gamboni, Andrew Bach, Stephen Chen, Weichun Chen, Peng Geng, Christopher T. Jagoe, Frederick R. Kinder, George T. Lee, Joseph McKenna, Timothy M. Ramsey, Oljan Repič, Larry Rogers, Wen-Chung Shieh, Run-Ming Wang, Liladhar Waykole
Publikováno v:
Organic Process Research & Development. 8:107-112
Autor:
Lech Ciszewski, Thomas J. Blacklock, Wenming Liu, Xu David, Kapa Prasad, Kevin Vargas, Oljan Repic, Liladhar Murlidhar Waykole, Joanna Szewczyk, George T. Lee, Calienni John Vincent
Publikováno v:
Organic Process Research & Development. 7:856-865
An optimized, convergent, safe synthesis of LAF389 (9), an anti-cancer agent analogous to bengamide B, is described. Starting from α-d-glucoheptonic (d-glycero-d-gulo-heptonic acid) γ-lactone (10), the lactone 15 was constructed in five steps. Majo
Autor:
Michael J. Girgis, George T. Lee, Apurva Chaudhary, James W. Streemke, Kapa Prasad, Oljan Repic
Publikováno v:
Organic Process Research & Development. 7:723-732
A process to prepare 2-propionyl-4-bromoaniline by ortho acylation of 4-bromoaniline under Sugasawa conditions was developed. Upon scale-up in a pilot plant, the process gave lower yields than in the laboratory in four out of five plant runs. Analysi
Autor:
Kau-Ming Chen, Mahavir Prashad, Oljan Repic, Carmine Villa, Kapa Prasad, Lech Ciszewski, George T. Lee, John C. Amedio
Publikováno v:
Organic Process Research & Development. 6:773-776
An efficient, safe, and cost-effective synthesis of 3-carboxy-(2R)-[[hydroxy[(tetradecyl)oxy]phosphinyl]oxy]-N,N,N-trimethyl-1-propanaminium hydroxide inner salt (1, CPI975), a carnitine palmitoyltransferase I inhibitor, is described. The reaction of