Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Jason W. B. Cooke"'
Publikováno v:
Organic Process Research & Development. 19:1954-1965
An improved process for the manufacture of (R)-3,5-bis(trifluoromethyl)-α-methyl-N-methylbenzylamine l-(−)-malic acid salt (1), a key starting material for many pharmaceutical targets, is described. Rapid process understanding for the synthesis of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::47040b9fb998dc6e90d5e1a82a3179c7
https://doi.org/10.1021/acs.oprd.5b00283
https://doi.org/10.1021/acs.oprd.5b00283
Autor:
Stacy Clark, Stephanie Q. Q. Ng, Jason W. B. Cooke, Benjamin I. Andrews, John C. S. Gray, Robert M. Harris
Publikováno v:
Organic Process Research & Development. 17:1239-1246
A fit for purpose approach has been adopted in order to develop a robust, scalable route to the S1P1 receptor agonist, GSK2263167. The key steps include a Robinson ring annulation followed by a Saegusa oxidation, providing rapid access to an advanced
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::711ee6de664c9e479240bef243d05491
https://doi.org/10.1021/op400162p
https://doi.org/10.1021/op400162p
Autor:
Sara Rossi, Davide Tramarin, William Maton, Brigida Allieri, Francesca Campi, Pieter Westerduin, Gilles Laval, Jason W. B. Cooke, Zadeo Cimarosti, Paolo Stabile, Nicola Giubellina
Publikováno v:
Organic Process Research & Development. 16:1598-1606
The studies carried out to develop a robust crystallization method for the substituted piperazinyl-quinoline (1) a compound potentially active in the treatment of depression, are described in this contribution. These studies include the control of a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7047d1fcd161eb000d8b634507416017
https://doi.org/10.1021/op300126e
https://doi.org/10.1021/op300126e
Autor:
Sara Rossi, Paolo Stabile, Jason W. B. Cooke, Gilles Laval, Paola Russo, Roberta Pachera, Ramona Moretti, Pieter Westerduin, Zadeo Cimarosti, Nicola Giubellina, Francesco Tinazzi, William Maton
Publikováno v:
Organic Process Research & Development. 15:1287-1296
1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone, 1, was identified as a potential drug for the treatment of depression and anxiety. Herein is described the work carried out to select the manufacturing route and the pr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f192f5af1e4d746b5fb7e9edfa63ad2c
https://doi.org/10.1021/op200140v
https://doi.org/10.1021/op200140v
Autor:
Andrea C. Haynes, Benjamin I. Andrews, Bela Rajiv Patel, Jason Witherington, Mary A. Morse, Umesh Kumar, Colin A. Campbell, Pam Gaskin, Sapna Desai, Robert Willis, Jason W. B. Cooke, Greg J. Osborne, Simon Taylor, Robert J. Watson, Terry Panchal, Alcide Perboni, Nigel Deeks, James Gray, Simon J. Dowell, Duncan S. Holmes, Rino A. Bit, Emmanuel Hubert Demont
Publikováno v:
ACS Medicinal Chemistry Letters. 2:444-449
Gilenya (fingolimod, FTY720) was recently approved by the U.S. FDA for the treatment of patients with remitting relapsing multiple sclerosis (RRMS). It is a potent agonist of four of the five sphingosine 1-phosphate (S1P) G-protein-coupled receptors
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63c6ce69eae4fc0f23f898780b99469f
https://doi.org/10.1021/ml2000214
https://doi.org/10.1021/ml2000214
Autor:
Pieter Westerduin, Alcide Perboni, Zadeo Cimarosti, Gilles Laval, Paolo Stabile, Jason W. B. Cooke, Nicola Giubellina
Publikováno v:
Organic Process Research & Development. 14:859-867
The development and scale-up of an optimized synthesis for a novel drug candidate for depression and anxiety is presented. The updated synthesis represents a convergent and efficient four-stage app...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a849e4d9e4ea3d5c744984d16434a0ec
https://doi.org/10.1021/op100103v
https://doi.org/10.1021/op100103v
Publikováno v:
Synlett. 2010:618-622
In this paper we present a study into the direct formation of five plant-derived natural products via intramolecular Diels-Alder cycloaddition of a series of 1,7,9-decatriene precursors. Methods for the preparation of the trienes are also discussed.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f1daa38ee6d3615c3792946c4c15c83b
https://doi.org/10.1055/s-0029-1219158
https://doi.org/10.1055/s-0029-1219158
Autor:
Peter W. Scott, Åsa Sjolin, Ron M. Lawrence, Jason W. B. Cooke, Roger Barrett, Darren Caine, Kevin S. Cardwell
Publikováno v:
Tetrahedron: Asymmetry. 14:3627-3631
A convenient, efficient and cost-effective two-stage synthesis of benzyl (3R)-3-amino-2-oxo-1-pyrrolidinecarboxylate (2S,3S)-2,3-bis[(4-methylbenzoyl)oxy]butanediote (2:1) via a crystallisation-induced dynamic resolution process is reported.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e7e3fe7453d939e07fcbd98ec8435bb1
https://doi.org/10.1016/s0957-4166(03)00546-9
https://doi.org/10.1016/s0957-4166(03)00546-9
Publikováno v:
Organic Process Research & Development. 5:383-386
Eniluracil (5-ethynyluracil) is a potent inactivator of the enzyme dihydropyrimidine dehydrogenase, which is the rate-limiting enzyme in the metabolism of 5-fluorouracil, a widely used anti-cancer drug. The process research and development of a three
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::59e9f000bb19ad504fcb39967413cf01
https://doi.org/10.1021/op0100100
https://doi.org/10.1021/op0100100
Publikováno v:
Organic Process Research & Development. 5:37-44
A new method for the synthesis of 2,4-disubstituted oxazoles and thiazoles and 2,4,5-trisubstituted oxazoles from readily available starting materials is described. The methodology has been applied on multigram scale and involves transfer of oxidatio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2d795aba12638467756e7a98703e1e9b
https://doi.org/10.1021/op000086g
https://doi.org/10.1021/op000086g