Development of an Intrinsically Safer Methanolysis/Aromatic Nitro Group Reduction for Step 1 and 2 of Talazoparib Tosylate

Autor: Steven J. Fussell, Craig J. Knight, Michael Hawksworth, Daniel Laity, Suju Mathew, Samantha V. Oke, Philip Peach, David S. B. Daniels, Olivier Dirat, Robert Crook, Adam Gymer, Samantha Prior

Publikováno v: Organic Process Research & Development. 25:2686-2692

A change in facility for the synthesis of the step 2 intermediate for talazoparib tosylate (1·TsOH) required the development of an alternative, intrinsically safer process. Rapid route scouting and...

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1124bef7ea76a5fb8e305d8553bf7b96
https://doi.org/10.1021/acs.oprd.1c00259

Optimizing the Mizoroki–Heck reaction of cyclic allyl amines: Gram-scale synthesis of preclamol without protecting groups

Autor: Kirsty Adams, Bimod Thapa, Fanny Tran, Joseph B. Sweeney, Robert Crook, Julien Doulcet

Publikováno v: Journal of Catalysis. 360:97-101

Though a widely used metal-catalyzed cross-coupling process, the Mizoroki–Heck (MH) reaction can be a capricious transformation. This is particularly true for oxidation-prone alkene substrates containing ligating heteroatoms, as in the case of N-al

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::da96948133f56f9b34124141186d5815
https://doi.org/10.1016/j.jcat.2018.01.007

A comparative study of amide-bond forming reagents in aqueous media – Substrate scope and reagent compatibility

Autor: Matthew Badland, Roger M. Howard, Steven J. Fussell, Robert Walton, Gerald A. Weisenburger, Bastien Delayre, Iain Robert Gladwell, Michael Hawksworth, Robert Crook

Publikováno v: Tetrahedron Letters. 58:4391-4394

A survey of amidation reagents demonstrating DIC-HOPO, DMT-MM, COMU-collidine, TPTU-NMI, EEDQ, CDI and EDC-Oxyma to be effective for the coupling of carboxylic acids with amines in the presence of water and the absence of problematic dipolar aprotic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b2c23889f736cc9b056d154aea3a1d37
https://doi.org/10.1016/j.tetlet.2017.10.014

Biocatalytic Routes to Enantiomerically Enriched Dibenz[c,e]azepines

Autor: Scott P. France, Godwin A. Aleku, Mahima Sharma, Juan Mangas-Sanchez, Roger M. Howard, Jeremy Steflik, Rajesh Kumar, Ralph W. Adams, Iustina Slabu, Robert Crook, Gideon Grogan, Timothy W. Wallace, Nicholas J. Turner

Publikováno v: France, S P, Aleku, G A, Sharma, M, Mangas-Sanchez, J, Howard, R M, Steflik, J, Kumar, R, Adams, R W, Slabu, I, Crook, R, Grogan, G, Wallace, T W & Turner, N J 2017, ' Biocatalytic Routes to Enantiomerically Enriched Dibenz[c,e]azepines ', Angewandte Chemie-International Edition, vol. 56, no. 49, pp. 15589-15593 . https://doi.org/10.1002/anie.201708453
Angewandte Chemie

Biocatalytic retrosynthetic analysis of dibenz[c,e]azepines has highlighted the use of imine reductase (IRED) and ω-transaminase (ω-TA) biocatalysts to establish the key stereocentres of these molecules. Several enantiocomplementary IREDs were iden

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c1f3d360b35495927371b1aab0a9d5a
https://eprints.whiterose.ac.uk/123887/1/Accepted_Manuscript.docx

Discovery and synthesis of a new class of opioid ligand having a 3-azabicyclo[3.1.0]hexane core. An example of a ‘magic methyl’ giving a 35-fold improvement in binding

Autor: Yogesh A. Sabnis, Alan John Pettman, Bernard Joseph Banks, Neil Feeder, Robert Crook, Graham Lunn

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:4608-4611

In looking for a novel achiral μ opioid receptor antagonist for the treatment of pruritus, we designed and synthesised azabicyclo[3.1.0]hexane compounds as a new class of opioid ligand. During optimisation, an addition of a single methyl resulted in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a0e297263a99c7bdbaee7eefac415c3a
https://doi.org/10.1016/j.bmcl.2011.05.132