Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Daniel Terence Tape"'
Publikováno v:
Organic & Biomolecular Chemistry. 16:6663-6674
2-Spiropiperidines are a highly desirable, yet under represented structure in drug discovery. 2-Spiropiperidines were synthesised in either a two-pot or one-pot reaction. In the two-pot reaction, the addition of a Weiler dianion to N-Boc imines, foll
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e96293ddde0ef863ce28e82cafea6651
https://doi.org/10.1039/c8ob01272e
https://doi.org/10.1039/c8ob01272e
Publikováno v:
Organic & Biomolecular Chemistry. 16:6620-6633
Spiropiperidines have gained in popularity in drug discovery programmes as medicinal chemists explore new areas of three-dimensional chemical space. This review focuses on the methodology used for the construction of 2-, 3- and 4- spiropiperidines, c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cbc90e3dd7f06d5b923e51ca37f38650
https://doi.org/10.1039/c8ob01271g
https://doi.org/10.1039/c8ob01271g
Publikováno v:
Synthesis. 49:3775-3793
The regioselective synthesis of 3-aminoimidazo[1,2-a]pyrimidines via triflic anhydride mediated amide activation and intramolecular cyclisation is reported. The nature of the added pyridine base allows access to both regioisomers from a simple common
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a04f81ee942f2d34e705eb4c3d324410
https://doi.org/10.1055/s-0036-1588425
https://doi.org/10.1055/s-0036-1588425
Publikováno v:
Organicbiomolecular chemistry. 16(36)
Correction for ‘Synthesis of highly substituted 2-spiropiperidines’ by Samuel D. Griggs et al., Org. Biomol. Chem., 2018, DOI: 10.1039/c8ob01272e.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e396c8df466c02390c57d2859346fa0
https://pubmed.ncbi.nlm.nih.gov/30067258
https://pubmed.ncbi.nlm.nih.gov/30067258
A general two-step synthesis of 2-spiropiperidines has been developed. δ-Amino-β-ketoesters can be reacted with cyclic ketones to generate 2-spiropiperidines in good to excellent yields. The 2-spiropiperidines formed occupy an under-explored region
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::774656eb219e40ba1a623f37cb347612
https://eprints.whiterose.ac.uk/117150/1/Final_Clarke_2_spiropiperidine.docx
https://eprints.whiterose.ac.uk/117150/1/Final_Clarke_2_spiropiperidine.docx
Autor:
Heather Hobbs, Rick P. C. Cousins, Caroline Whitworth, Ruth R. Osborn, Cesar Ramirez-Molina, Giorgia Vicentini, Chris Ioannou, Chun-wa Chung, Jeremy John Payne, Michelle L. Heathcote, Michael David Barker, Sebastien Andre Campos, Paul Faulder, Mary A. Morse, William L. Rumsey, John Liddle, Daniel Terence Tape, John Martin Pritchard, Rick Williamson, Duncan S. Holmes, Paul Bamborough
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5222-5226
The lead optimization of a series of potent azaindole IKK2 inhibitors is described. Optimization of the human whole blood activity and selectivity over IKK1 in parallel led to the discovery of 16, a potent and selective IKK2 inhibitor showing good ef
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::66c01094b7cd1f9f02ade498d99ac86e
https://doi.org/10.1016/j.bmcl.2012.06.065
https://doi.org/10.1016/j.bmcl.2012.06.065
Autor:
Andrew J. Burton, Mark B. Schilling, Keith Mills, Richard A. Henson, Fiona M. Adam, Daniel Terence Tape, Richard Cox, Jeremy C. Prodger, Kevin S. Cardwell
Publikováno v:
Tetrahedron Letters. 44:5657-5659
New syntheses of the amino-1,2,4-triazine, GW356194 have been developed to improve on existing methodology. The use of different amidrazones in cyclisations with α-keto and α-amido carbonyl compounds as the key step for the synthesis of the 1,2,4-t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::79aeda7f28b4e559629fd298e2973eeb
https://doi.org/10.1016/s0040-4039(03)01359-5
https://doi.org/10.1016/s0040-4039(03)01359-5
Autor:
Jeremy John Payne, Geoff W. Mellor, Smith Kathryn Jane, Richard A. Williamson, Sebastien Andre Campos, Geoffrey J. Cutler, Caroline Whitworth, Mary A. Morse, Michael David Barker, Heather Hobbs, Rick P. C. Cousins, Duncan S. Holmes, Daniel Terence Tape, Paul Bamborough, John Martin Pritchard, John Liddle, Chris Ioannou
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(9)
The synthesis and SAR of a novel series of IKK2 inhibitors are described. Modification around the hinge binding region of the 7-azaindole led to a series of potent and selective inhibitors with good cellular activity.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bac9d3089c47e68ac4f0cac67941fe59
https://pubmed.ncbi.nlm.nih.gov/19349179
https://pubmed.ncbi.nlm.nih.gov/19349179