Optimization of Imidazo[4,5-b]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical …

…, N Brown, PW Sheldrake… - Journal of medicinal …, 2012 - ACS Publications
Optimization of the imidazo[4,5-b]pyridine-based series of Aurora kinase inhibitors led to the
identification of 6-chloro-7-(4-(4-chlorobenzyl)piperazin-1-yl)-2-(1,3-dimethyl-1H-pyrazol-4-…

Total synthesis of erythromycins. 4. Total synthesis of erythronolide B

…, EJ Trybulski, R Lett, PW Sheldrake - Journal of the …, 1978 - ACS Publications
with 2-methoxypropene16 in CCU in the presence of a trace of phosphorus oxychloride and
exposed to 3 equiv of lithium acetylide-ethylenediamine complex in dimethyl sulfoxide at 25 …

Conformation analyses, dynamic behavior and amide bond distortions of medium-sized heterocycles. 1. Partially and fully reduced 1-benzazepines

M Qadir, J Cobb, PW Sheldrake, N Whittall… - The Journal of …, 2005 - ACS Publications
Five 1-benzazepine heterocycles were synthesized by utilizing transition-metal-catalyzed
processes in key bond-forming steps. exo-Methylene and methyl substituents were introduced …

Total synthesis of erythromycins. 3. Stereoselective routes to intermediates corresponding to C (1) to C (9) and C (10) to C (13) fragments of erythronolide B

…, JA Secrist, R Lett, PW Sheldrake… - Journal of the …, 1978 - ACS Publications
These results indicated that theadenine ring was constituted from two molecules of formamide
and three molecules of hydrogen cyanide. Among the CN units in adenine, C5-N7, Ce-…

Facile generation of a library of 5-aryl-2-arylsulfonyl-1, 3-thiazoles

PW Sheldrake, M Matteucci, E McDonald - Synlett, 2006 - thieme-connect.com
Abstract Treatment of N, N-diformylaminomethyl aryl ketones with phosphorus pentasulfide/triethylamine
in chloroform gives 5-arylthiazoles directly in good yield. The 5-aryl-1, 3-…

An efficient method for the synthesis of substituted TosMIC precursors

J Sisko, M Mellinger, PW Sheldrake, NH Baine - Tetrahedron letters, 1996 - Elsevier
Substituted tosylmethyl isocyanides (TosMICs) are useful reagents for which no general method
of preparation is available. We describe here a high-yielding method for the synthesis of …

Synthesis of 2-substituted 1-benzyl-2, 3, 4, 5-tetrahydro-1-benzazepines by palladium catalysis. Observation of a competitive β-hydride elimination pathway

…, T Gelbrich, SJ Coles, MB Hursthouse, PW Sheldrake… - Tetrahedron letters, 2003 - Elsevier
A synthetic route to 1-benzyl-tetrahydro-1-benzazepine is reported, which also permits access
to analogous structures with alkyl and aryl substituents at position-2 of the aliphatic ring. …

The phosphoinositide-specific phospholipase C inhibitor U73122 (1-(6-((17β-3-methoxyestra-1, 3, 5 (10)-trien-17-yl) amino) hexyl)-1H-pyrrole-2, 5-dione) …

…, YM Newbatt, W Aherne, PW Sheldrake… - Drug metabolism and …, 2007 - ASPET
Phosphoinositide-specific phospholipase C (PLC) is a key enzyme in the regulation of Ca 2+
release from inositol 1,4,5-triphosphate-sensitive stores. U73122 (1-(6-((17β-3-…

Conformation analyses, dynamic behavior, and amide bond distortions of medium-sized heterocycles. 2. Partially and fully reduced 1-benzazocines, benzazonines …

M Qadir, J Cobb, PW Sheldrake, N Whittall… - The Journal of …, 2005 - ACS Publications
Partially and fully reduced forms of benzo-fused eight- to ten-membered nitrogen
heterocycles (1-benzazecines, 1-benzazonines and 1-benzazecines) have been prepared. …

Synthesis of SB-214857 using copper catalysed amination of arylbromides with L-aspartic acid

JB Clement, JF Hayes, HM Sheldrake, PW Sheldrake… - Synlett, 2001 - thieme-connect.com
An efficient synthesis of a 1, 4-benzodiazepine was accomplished using copper catalysed
amination of an arylbromide with the soluble bis-tetrabutylammonium salt of L-aspartic acid …