Survey of Solvent Usage in Papers Published in Organic Process Research & Development 1997–2012
- Christopher P. Ashcroft, P. Dunn, J. Hayler, A. Wells
- Chemistry
- 6 February 2015
A survey of solvent usage for papers published in Organic Process Research & Development has been carried out for the years 1997–2012. Three solvent categories were studied: (i) solvents of concern,…
Second-Generation Process Research Towards Eletriptan: A Fischer Indole Approach
- Christopher P. Ashcroft, Paul C. Hellier, A. Pettman, S. Watkinson
- Chemistry, Business
- 21 January 2011
The development of a second-generation process for the synthesis of eletriptan via a Fischer indole cyclisation is described. The finalised process offers several potential advantages over the…
Asymmetric Synthesis of an MMP-3 Inhibitor Incorporating a 2-Alkyl Succinate Motif
- Christopher P. Ashcroft, S. Challenger, A. Derrick, R. Storey, N. Thomson
- Chemistry
- 22 March 2003
An efficient and practical synthesis is presented of the pharmaceutically active MMP-3 inhibitor UK-370,106 (1) via an olefination/catalytic asymmetric hydrogenation sequence. Commercially available…
Discovery of an HIV integrase inhibitor with an excellent resistance profile
- D. Pryde, R. Webster, R. A. Bissell
- Biology, Chemistry
- 27 March 2013
SAR studies within a series of N-hydroxy-dihydronaphthyridinone HIV integrase inhibitors led to a candidate compound, PF-4776548, of high potency and with an excellent resistance profile, which was taken into a human microdose study to confirm its human pharmacokinetics.
An Efficient and Scalable Synthesis of the Endothelin Antagonists UK-350,926 and UK-349,862 Using a Dynamic Resolution Process
- Christopher P. Ashcroft, S. Challenger, J. Williams
- Chemistry
- 19 August 2005
The development and scale-up of a potential manufacturing route to the endothelin antagonists UK-350,926 1 and UK-349,862 2 are described. A key synthetic challenge in designing an efficient route to…
Route Selection and Process Development of a Multikilogram Route to the Inhaled A2a Agonist UK-432,097
- Christopher P. Ashcroft, Yann Dessi, D. Entwistle, Lynsey C. Hesmondhalgh, Adrian Longstaff, J. D. Smith
- Chemistry
- 29 February 2012
This article describes the selection, process development, and scale-up of a synthetic route to a complex nucleoside analogue, the A2a agonist UK-432,097 (1), that culminated in the manufacture of…
Catalyst controlled regioselective Suzuki cross-coupling of 2-(4-bromophenyl)-5-chloropyrazine
- Christopher P. Ashcroft, Steven J. Fussell, K. Wilford
- Chemistry
- 21 August 2013
Cu-Catalyzed Hydroboration of Benzylidenecyclopropanes: Reaction Optimization, (Hetero)Aryl Scope, and Origins of Pathway Selectivity.
- Jose M. Medina, Tae-Ah Kang, K. Engle
- Chemistry, BiologyACS Catalysis
- 28 June 2019
The copper-catalyzed hydroboration of benzylidenecyclopropanes, conveniently accessed in one step from readily available benzaldehydes, is reported, giving access to valuable synthetic intermediates.
Catalyst Controlled Regioselective Suzuki Cross-Coupling of 2-(4-Bromophenyl)-5-chloropyrazine.
- Christopher P. Ashcroft, Steven J. Fussell, K. Wilford
- Chemistry
- 17 December 2013
The Suzuki cross-coupling between 2-(4-bromophenyl)-5-chloropyrazine (I) and a range of aryl boronic acids is investigated.
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