441044-12-8Relevant articles and documents
QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS
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Page/Page column 79-82, (2008/06/13)
The invention concerns quinazoline derivatives of the Formula (I), or pharmaceutically acceptable salts thereof: I wherein each of R1, R2, R3, R4 and m are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula (I) are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.
Use of hydrolases for the synthesis of cyclic amino acids
Lloyd, Richard C.,Lloyd, Michael C.,Smith, Mark E. B.,Holt, Karen E.,Swift, Jonathan P.,Keene, Philip A.,Taylor, Stephen J. C.,McCague, Raymond
, p. 717 - 728 (2007/10/03)
The synthesis of several cyclic amino acids that have all the necessary structural features to make them ideal scaffolds for use in medicinal chemistry is described. A key step in each synthesis is the use of hydrolase enzymes to define a chiral centre. I
Chemoenzymatic synthesis of the four diastereoisomers of 4-hydroxypipecolic acid from N-acetyl-(R,S)-allylglycine: Chiral scaffolds for drug discovery
Lloyd, Richard C.,Smith, Mark E. B.,Brick, Dean,Taylor, Stephen J. C.,Chaplin, David A.,McCague, Raymond
, p. 762 - 766 (2013/09/06)
All four diastereoisomers of 4-hydroxypipecolic acid were prepared in a form conveniently protected for drug discovery applications with the use of industrially scaleable methodology. Resolution of the racemic starting material using proprietary acylases followed by an acyliminium ion cyclisation gave diastereomeric mixtures of 4-formyloxypipecolic acid, which were differentiated using an enzyme-catalysed hydrolysis. The products were separated by partition, and by following a sequence of straightforward chemical steps, the individual stereoisomers of the protected 4-hydroxypipecolates were crystallized to optical purity in 100 g quantities.
