Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Faye J. Sheen"'
Autor:
Sarah E. Brewer, Ed Cleator, Debra J. Wallace, Paulo Avalle, Jeremy P. Scott, Andrew D. Gibb, Faye J. Sheen, Matthew M. Bio, Antony J. Davies, Gavin W. Stewart, Robert D. Wilson
Publikováno v:
Organic Process Research & Development. 17:1561-1567
The process development and multikilogram preparation of a TRPV1 antagonist, 1, is described. Pyrido[2,3-b]pyrazine 1 was prepared in a convergent manner by the coupling of two key fragments, glyoxal 2 and diamine 3. Glyoxal 2 was synthesized in six
Autor:
Brian C. Bishop, Mark McLaughlin, Jingjun Yin, Ed Cleator, Cheng Chen, Faye J. Sheen, Adrian Goodyear, Yingju Xu, Gavin W. Stewart, Xin Linghu
Publikováno v:
Organic Process Research & Development. 16:605-611
A new synthetic route has been developed to drug candidate 1, a second-generation NNRTI being developed as a potential treatment of HIV. Regiocontrol in a key alkylation step was achieved by selective N-alkylation of hydrazone 13. After a deprotectio
Autor:
Faye J. Sheen, Neil A. Strotman, Carl A. Baxter, Robert A. Reamer, Debra J. Wallace, Ed Cleator, Karel M. J. Brands, Gavin W. Stewart, John S. Edwards
Publikováno v:
Organic Process Research & Development. 15:367-375
A new synthetic route to drug candidate 1, a potent and selective dual orexin antagonist for the treatment of sleep disorders, has been developed. The key acyclic precursor 10 was prepared in a one-step process in 75% isolated yield from commercially
Autor:
Michael P. O'Hagan, Gavin W. Stewart, Ed Cleator, Carl A. Baxter, Timothy J. C. O'Riordan, Faye J. Sheen
Publikováno v:
Tetrahedron Letters. 51:1079-1082
A simple one-pot synthesis of benzoxathiazepine-1,1-dioxides is described. Increased yields are afforded when suitable substituents are present in one of the starting materials. These additional substituents also provide a handle for further function
Autor:
Robert D. Wilson, Matthew M. Bio, Antony J. Davies, Faye J. Sheen, Andy Lawrence, Gavin W. Stewart, Ed Cleator, Simon E. Hamilton
Publikováno v:
Tetrahedron. 65:8950-8955
The development of a synthetically useful, regioselective cross-coupling of 2,4-diaminopyridines with aryl and heteroaryl halides is reported. Selectivity for coupling through either amine is controlled by a simple change in the reaction conditions.
Autor:
Robert D. Wilson, George Zhou, Antony J. Davies, Gavin W. Stewart, Karel M. J. Brands, David Hands, Steven F. Oliver, Michael S. Ashwood, Robert A. Reamer, Ed Cleator, Matthew M. Bio, Ulf-H. Dolling, Khateeta M. Emerson, Faye J. Sheen, Arlene E. Mckeown, Andrew D. Gibb
Publikováno v:
Organic Process Research & Development. 13:543-547
A practical and efficient synthesis of 1,4,5,6-tetrahydro-3-(1H-tetrazol-5-yl)cyclopenta[c]pyrazole, 1, is described. A new one-pot process has been developed, starting from the commercially availa...
Autor:
Ulf-H. Dolling, Antony J. Davies, K. M. Jos Brands, Matthew M. Bio, Faye J. Sheen, Ed Cleator
Publikováno v:
Tetrahedron Letters. 47:4245-4248
A novel and efficient synthesis of a range of racemic and enantioenriched N-substituted-4-substituted isothiazolidine-1,1-dioxides from epoxides and sulfonamides is described. The critical choice of the activating group for the cyclization event is d
Autor:
Antony J. Davies, Karel M. J. Brands, Sarah E. Brewer, Robert D. Wilson, Jeremy P. Scott, Andrew D. Gibb, Faye J. Sheen, Ulf-H. Dolling, David Hands, Stephen P. Keen, Robert A. Reamer, Steven F. Oliver
Publikováno v:
The Journal of Organic Chemistry. 71:3086-3092
A practical asymmetric synthesis of the gamma-secretase inhibitor (-)-1 is described. As the key transformation, a highly diastereoselective intramolecular nitrile oxide cycloaddition forms the hexahydrobenzisoxazole core of 3 in four operations. Oth
Autor:
Ed Cleator, Michael P. O'Hagan, Gavin W. Stewart, Faye J. Sheen, Timothy J. C. O'Riordan, Carl A. Baxter
Publikováno v:
ChemInform. 41
A simple one-pot synthesis of benzoxathiazepine-1,1-dioxides is described. Increased yields are afforded when suitable substituents are present in one of the starting materials. These additional substituents also provide a handle for further function
Autor:
Antony J. Davies, Andy Lawrence, Matthew M. Bio, Robert D. Wilson, Ed Cleator, Gavin W. Stewart, Simon E. Hamilton, Faye J. Sheen
Publikováno v:
ChemInform. 41
The development of a synthetically useful, regioselective cross-coupling of 2,4-diaminopyridines with aryl and heteroaryl halides is reported. Selectivity for coupling through either amine is controlled by a simple change in the reaction conditions.