27041 Catalytic methods for preparation of chiral amines
Researchers at the University of Sheffield have developed and optimised new systems for the preparation of chiral amines in almost quantitative yield and as, essentially, one stereoisomer.
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The worldwide pharmaceutical and fine chemical industry has an increasing need for more efficient and selective methods for the construction of molecules of high commercial value. However, many organic, biochemical and biological compounds are chiral (that is they have a structure that cannot be superimposed on its mirror image) which, when used as pharmaceuticals, can differ markedly in their efficacy or toxicity. Additionally, strict regulatory procedures introduced after previous problems with pharmaceutical stereo isomers) now dictate that any chiral compounds (existing as two enantiomeric molecules) must be evaluated in both of these forms. This has led to an enormous global interest in developing new methods and techniques for the production of chiral molecules. Controlling the chirality of the final product using current methods is complicated and involves a great deal of optimisation of many different factors which affect the outcome of the catalytic process, such as the catalyst structure, catalyst loading, solvent, temperature and time. Relatively minor changes in any one of these factors can have a significant and often detrimental effect on the stereo chemical outcome of the reaction.
Researchers at the University of Sheffield have developed and optimised new systems for the preparation of chiral amines in almost quantitative yield and as, essentially, one stereoisomer. Their system is also unique since it allows a ‘one-pot’ two-step transformation, operating efficiently with only 1% of catalyst compared to those reported in the literature, which require 10%. These catalysts also have the advantage of being easily prepared and do not require transition metals, which can be expensive and can contaminate the end product.
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