Heal J.,Prosarix Ltd. |
Brough S.,Key Organics Ltd.
Sp2 | Year: 2014
KeyFinder libraries have been developed by Key Organics in partnership with Prosarix to provide a cutting-edge service to support early-phase drug discovery.
Lee D.S.,University of Nottingham |
Amara Z.,University of Nottingham |
Poliakoff M.,University of Nottingham |
Harman T.,Aesica Pharmaceuticals |
And 5 more authors.
Organic Process Research and Development | Year: 2015
Methods for the batch scale up of DABAL-Me3 promoted direct ester to amide synthesis have been demonstrated at 10-100 g scales using a tert-amide model compound. Procedures for 20 g scale couplings in standard laboratory glassware and up to 0.1 kg in industry-standard jacketed glass reactors in near quantitative yields are given. A derivative of the anticancer agent Imatinib (Gleevec) has been synthesized on a 26 g scale (98% yield, >98% purity) establishing DABAL-Me3 as a potential alternative for the synthesis of amides in API scale preparations. Continuous flow methodology provides a method for larger scales (productivities of >50 g h-1). In addition, nitriles were coupled to primary amines and hydrazines with DABAL-Me3, resulting in the clean formation of free amidines (16 examples) and amidrazones. © 2015 American Chemical Society.
Olkhov R.V.,University of Exeter |
Parker R.,University of Exeter |
Parker R.,Key Organics Ltd. |
Shaw A.M.,University of Exeter
Biosensors and Bioelectronics | Year: 2012
A gold nanoparticle, localised plasmon array biosensor using light scattering has been employed in the detection of allergen-specific antibodies in whole blood and sera. The array sensor was functionalized with four different allergens, cat dander (Fel d1), dust mite (Der p1), peanut allergen (Ara h1) and dog dander (Can f1) and immuno-kinetic assay was performed to detect their respective anti-allergen IgG antibodies. Specific positive responses to antibodies at a concentration of 25. nM were observed for Fel d1, Der p1, and Ara h1 allergens, while the Can f1 channel served as a reference control. The sensitivity was further enhanced using a secondary anti-IgG detection antibodies to give a limit of detection of 2. nM. The results indicate the potential for nanoparticle scattering multiplexed arrays to screen unprepared blood samples at point-of-care for assays of complex samples such as the whole blood. © 2012.
Carey J.V.,Key Organics Ltd.
Chimica Oggi/Chemistry Today | Year: 2014
The number of commercially available chiral bisphosphine ligands has grown substantially in the last decade, which has resulted in an increased range of applications in asymmetric chemocatalysis, together with improved enantioselectivity, higher S/C ratio's and milder reaction conditions. However, the majority of new ligands introduced are variations of the C2 axially symmetrical BINAP or DIOP, which contain a chiral backbone. In comparison, the synthesis of new P-chiral bisphosphines, based on the pioneering DIPAMP ligand, is noteworthy because fewer new examples of this structural class have been introduced and utilised.
Haydon D.J.,Biota Europe Ltd |
Bennett J.M.,Biota Europe Ltd |
Brown D.,Biota Europe Ltd |
Collins I.,Biota Europe Ltd |
And 14 more authors.
Journal of Medicinal Chemistry | Year: 2010
3-Methoxybenzamide (1) is a weak inhibitor of the essential bacterial cell division protein FtsZ. Alkyl derivatives of 1 are potent antistaphylococcal compounds with suboptimal drug-like properties. Exploration of the structure-activity relationships of analogues of these inhibitors led to the identification of potent antistaphylococcal compounds with improved pharmaceutical properties. © 2010 American Chemical Society.