Zobrazeno 1 - 10
of 43
pro vyhledávání: '"Dalian, Zhao"'
Autor:
Michel Journet, Zhihui Peng, Dalian Zhao, Arlene E. Mckeown, Guy R. Humphrey, Jeffrey T. Kuethe
Publikováno v:
Organic Process Research & Development. 20:227-232
A highly efficient, regioselective five-step synthesis of the TRPV1 antagonist 1 is described. The coupling of piperazine 7 with dichloropyrimidine 8 proceeded via a regioselective Pd-mediated amination affording product 11 in excellent yield. Conver
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9ff56dfdcc1dda616fbcb2bfe14089a9
https://doi.org/10.1021/acs.oprd.5b00388
https://doi.org/10.1021/acs.oprd.5b00388
Autor:
Wynne V. Kandur, Dalian Zhao, Mark A. Huffman, Ed Cleator, Mary M. Kim, Gavin W. Stewart, Rebecca T. Ruck
Publikováno v:
Organic Process Research & Development. 16:1329-1337
Route development and demonstration on multikilogram scale for the first GMP delivery of MK-4256 are described. Key aspects of the convergent route include a regioselective green iodination, one-pot oxadiazole synthesis, and an efficient ketone Picte
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::56f3b692fcc77525e04e7e4e1acfa177
https://doi.org/10.1021/op300128c
https://doi.org/10.1021/op300128c
Autor:
R. Scott Hoerrner, Juan D. Arredondo, C. Scott Shultz, Takahiro Itoh, Xianghui Wen, Debra J. Wallace, Jason L. Nyrop, Dalian Zhao, Paul G. Bulger, Daniel J. Muzzio, Lushi Tan, Ephraim M. Bassan, Qinghao Chen, Mark Weisel, Sarah J. Dolman, Chengfu Xie, Pintipa Grongsaard
Publikováno v:
Organic Process Research & Development. 16:1069-1081
The development of a convergent, chromatography-free synthesis of an allosteric Akt kinase inhibitor is described. The route comprised 17 total steps and was used to produce kilogram quantities of the target molecule. A key early transformation, for
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::317d3d594c7cd2a3aab48392e1bc47ab
https://doi.org/10.1021/op300031r
https://doi.org/10.1021/op300031r
Autor:
Ian W. Davies, Paul N. Devine, Robert A. Reamer, David M. Tschaen, Fei Zhang, Daniel Zewge, Jeffrey T. Kuethe, David R. Lieberman, Zhihui Peng, Kevin M. Belyk, David M. Tellers, Guy R. Humphrey, Peter G. Dormer, Michel Journet, Andrew Nolting, Marjorie S. Waters, Dalian Zhao, Zhiguo J. Song
Publikováno v:
The Journal of Organic Chemistry. 76:7804-7815
Development of a practical synthesis of MK-7009, a 22-membered macrocycle, is described. A variety of ring-closing strategies were evaluated, including ring-closing metathesis, intermolecular palladium-catalyzed cross-couplings, and macrolactamizatio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d1dc6683cb1f9b4cbaa077ffc9b2d32f
https://doi.org/10.1021/jo2011494
https://doi.org/10.1021/jo2011494
Autor:
Dalian Zhao, Michael C. Hillier, Shane W. Krska, Guy R. Humphrey, Edward J. J. Grabowski, Jean-François Marcoux, Peter E. Maligres
Publikováno v:
Organic Process Research & Development. 13:525-534
A practical, highly convergent, asymmetric synthesis of a selective PPARγ modulator 1 is described. The inhibitor contains two key components, a 6-trifluoromethoxy-3-acylindole (6) and (R)-α-aryloxybutanoic acid derivative (10). Two methods were de
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::18c346ff582dd3c89a6a3d2067c26457
https://doi.org/10.1021/op8002882
https://doi.org/10.1021/op8002882
Autor:
Richard D. Tillyer, Jean-François Marcoux, and Arlene E. McKeown, Dalian Zhao, Edward J. J. Grabowski, Michael C. Hillier
Publikováno v:
The Journal of Organic Chemistry. 70:8385-8394
A general asymmetric synthesis of substituted cycloalkyl[b]indoles has been accomplished. The key features of this approach are (1) the utilization of a Japp-Klingemann condensation/Fischer cyclization to prepare cycloalkyl[b]indolones, (2) the asymm
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::669580a38790abc14246394af15f7786
https://doi.org/10.1021/jo051146p
https://doi.org/10.1021/jo051146p
Autor:
Rob D. Larsen, Ralph P. Volante, Michel Journet, Ali Shafiee, Mirlinda Biba, Edward J. J. Grabowski, Anthony O. King, Jean-François Marcoux, Dalian Zhao, Veena Upadhyay, Kevin R. Campos, Edward G. Corley, Richard D. Tillyer
Publikováno v:
Tetrahedron: Asymmetry. 16:3094-3098
Three racemic esters including indole-ethyl ester 1 as well as its related derivatives 3 and 4 in Scheme 1, all synthetic intermediates for the preparation of chiral compound 5 , were used as substrates to evaluate the catalytic potentials of a panel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::fc31e420824bec11ba9c2331d75dc44d
https://doi.org/10.1016/j.tetasy.2005.08.021
https://doi.org/10.1016/j.tetasy.2005.08.021
Autor:
Edward J. J. Grabowski, Karen Marcantonio, Amélie Roy, Dalian Zhao, Lushi Tan, Lisa F. Frey, Cheng-yi Chen, Richard D. Tillyer, Philippe Dagneau, Paul D. O’Shea, Xin Wang, Robert A. Reamer, Weirong Chen
Publikováno v:
The Journal of Organic Chemistry. 70:3021-3030
A practical, chromatography-free catalytic asymmetric synthesis of a potent and selective PDE4 inhibitor (L-869,298, 1) is described. Catalytic asymmetric hydrogenation of thiazole ketone 5a afforded the corresponding alcohol 3b in excellent enantios
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f04f04a3c82fadcb9efea44c3f787ae1
https://doi.org/10.1021/jo048156v
https://doi.org/10.1021/jo048156v
Autor:
Maia M. Cherney, Dalian Zhao, Michael N.G. James, Spencer Knapp, Don J. Mahuran, Brian L. Mark
Publikováno v:
Journal of Molecular Biology. 327:1093-1109
In humans, two major beta-hexosaminidase isoenzymes exist: Hex A and Hex B. Hex A is a heterodimer of subunits alpha and beta (60% identity), whereas Hex B is a homodimer of beta-subunits. Interest in human beta-hexosaminidase stems from its associat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::066a9014d2dbf428ebc72054368b41c2
https://doi.org/10.1016/s0022-2836(03)00216-x
https://doi.org/10.1016/s0022-2836(03)00216-x
Autor:
Xin Wang, Weirong Chen, Lushi Tan, Paul J. Reider, Lisa F. Frey, Philippe Dagneau, Anthony O. King, Cheng-yi Chen, Richard D. Tillyer, Feng Xu, Edward J. J. Grabowski, Paul D. O’Shea, Dalian Zhao
Publikováno v:
Tetrahedron. 58:7403-7410
Two synthetic strategies to the COX-2 specific inhibitor 1 have been described that allowed its preparation in large quantities in 79% overall yield from (S)-2-hydroxy-2-methylbutyric acid. These studies have led to the identification of an efficient
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6cd182f902592f23e2a50832948894e6
https://doi.org/10.1016/s0040-4020(02)00826-8
https://doi.org/10.1016/s0040-4020(02)00826-8