Research record

Publications

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201 publications found

Journal article

The Synthesis of Bcr-Abl Inhibiting Anticancer Pharmaceutical Agents Imatinib, Nilotinib and Dasatinib

Deadman, B. J. Hopkin, M. D.; Baxendale, I. R.; Ley, S. V.

Org. Biomol. Chem. · 2013 · 11 · 1766–1800

Imatinib (1), nilotinib (2) and dasatinib (3) are Bcr-Abl tyrosine kinase inhibitors approved for the treatment of chronic myelogenous leukemia (CML). This review collates information from the journal and patent literature to provide a comprehensive reference…

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Journal article

The Synthesis of Neurotensin Antagonist SR 48692 for Prostate Cancer Research

Baxendale, I. R.; Cheung, S.; Kitching, M. O.; Ley, S. V. Shearman, J. W.

Bioorg. Med. Chem. · 2013 · 21 · 4378–4387

An improved synthesis of the molecule SR 48692 is presented and its use as a neurotensin antagonist biological probe for use in cancer research is described. The preparation includes an number of enhanced chemical conversions and strategies to overcome some…

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Journal article

A "Catch–React–Release" Method for the FlowSynthesis of 2-Aminopyrimidines and Preparation of the Imatinib Base

Ingham, R. J.; Riva, E.; Nikbin, N.; Baxendale, I. R.; Ley, S. V.

Org. Lett. · 2012 · 14 · 3920–3923

The development of a monolith-supported synthetic procedure is reported, taking advantage of flow processing and the superior flow characteristics of monolithic reagents over gel-phase beads, to allow facile access to an important family of 2-aminopyrimidine …

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Journal article

A Flow-Based Synthesis of 2-Aminoadamantane-2-carboxylic Acid

Battilocchio, C.; Baxendale, I. R.; Biava, M.; Kitching, M. O.; Ley, S. V.

Org. Process Res. Dev. · 2012 · 16 · 798–810

The development of a new, high-yielding, scalable and safe process for the preparation of 2-aminoadamantane-2-carboxylic acid (1) is described. This geminal, functionalized achiral amino acid has been reported to possess interesting biological activity as a t…

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Journal article

A Total Synthesis of Millingtonine A

Wegner, J.; Ley, S. V.; Kirschning, A.; Hansen, A.-L.; Montenegro Garcia, J.; Baxendale, I. R.

Org. Lett. · 2012 · 14 · 696–699

A total synthesis of millingtonine A, a diglycosylated alkaloid, has been accomplished. Millingtonine A possesses a unique racemic tricyclic core structure not known from any other natural or synthetic source until now. The synthesis features a key bond-form…

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Journal article

Continuous flow reaction monitoring using an on-line miniature mass spectrometer

Browne, D. L.; Wright, S.; Deadman, B.; Dunnage, S.; Baxendale, I. R.; Turner, R.; Ley, S. V.

Rapid Commun. Mass Spectrom. · 2012 · 26 · 1999–2010

A recently developed miniature electrospray ionisation mass spectrometer has been coupled to a preparative flow chemistry system in order to monitor reactive intermediates and competing reaction paths, screen starting materials, and optimise reaction conditio…

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Journal article

Establishing a flow process to coumarin-8-carbaldehydes as important synthetic scaffolds

Zak, J.; Ron, D.; Riva, E.; Harding, H. P.; Cross, B. C. S.; Baxendale, I. R.

Chem. Eur. J. · 2012 · 32 · 9901–9910

Despite their usefulness as fluorophores and synthetic precursors, efficient and reliable routes to coumarin-8-carbaldehydes are lacking. We describe here a high-yielding continuous flow synthesis that requires no manual intermediate purification or work-up, …

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Journal article

Flow Assisted Scale-up of C2-symmetric Chiral PyBox-Ligands

Battilocchio, C.; Baumann, M.; Baxendale, I. R.; Biava, M.; Kitching, M. O.; Ley, S. V.; Martin, R. E.; Ohnmacht, S. A.; Tappin, N. D. C.

Synthesis · 2012 · (4) · 635–647

A series of PyBox ligands were prepared from commercially available chelidonic acid by a multistep flow sequence using mesoreactor technology. A chloro group introduced onto the ligand scaffold was subsequently exploited to give amine derivatives ready for im…

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Journal article

Flow Microwave Technology and Microreactors in Synthesis

Baxendale, I. R.; Hornung, C.; Ley, S. V.; Munõz Molina, J. de M.; Wikstrom, A.

Aust. J. Chem. · 2012 · 66 · 131–144

A bespoke microwave reactor with a glass containment cell has been developed for performing continuous flow reactions under microwave heating. The prototype unit has been evaluated using a series of standard organic chemical transformations enabling scale-up …

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Graphical abstract for The Evolution of Immobilized Reagents and their Application in Flow Chemistry for the Synthesis of Natural Products and Pharmaceutical Compounds

Book chapter

The Evolution of Immobilized Reagents and their Application in Flow Chemistry for the Synthesis of Natural Products and Pharmaceutical Compounds

Myers, R. M.; Roper, K. A.; Baxendale, I. R.; Ley, S. V.

Modern Tools for the Synthesis of Complex Bioactive Molecules · 2012 · Chapter 11 · 359–394

Underpinning a healthy drug discovery and development programme is the ability to prepare large numbers of structurally diverse molecules. Developing innovative practical chemical techniques to achieve this goal has therefore become essential. Indeed, the inc…

Journal article

The molecular basis for selective inhibition of unconventional mRNA splicing by an IRE1-binding small molecule

Cross, B. C. S.; Bond, P. J.; Sadowski, P. G.; Jha, B. K.; Zak, J.; Goodman, J. M.; Silverman, R. H.; Neubert, T. A.; Baxendale, I. R.; Ron, D.; Harding, H. P.

PNAS · 2012 · 15 · E869–E878

IRE1 couples endoplasmic reticulum unfolded protein load to RNA cleavage events that culminate in the sequence-specific splicing of the Xbp1 mRNA and in the regulated degradation of diverse membrane-bound mRNAs. We report on the identification of a small mole…

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Journal article

The Oxygen-Mediated Synthesis of 1,3-Butadiynes in Continuous Flow: Using Teflon AF-2400 to Effect Gas/Liquid Contact.

Petersen, T. P.; Polyzos, A.; O'Brien, M.; Ulven, T.; Baxendale, I. R.; Ley, S. V.

ChemSusChem · 2012 · 5 · 274–277

The gas is always greener: A continuous flow Glaser-Hay coupling reaction system, mediated by molecular oxygen, is developed based on a tube-in-tube gas/liquid reactor/injector. The system uses a semi-permeable Teflon AF-2400 membrane to effect rapid gas/liqu…

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