New partnership in chiral catalysis

Welsh company Great Lakes Fine Chemicals has teamed up with Phoenix Chemicals to develop new, more cost effective processes for the production of pharmaceutical intermediates.

Under the terms of the collaboration, GLFC has licensed its proprietary Ruthenium BINAP catalyst to Phoenix. The companies are hoping to find ways to make chiral or single-enantiomer compounds that are difficult or expensive to produce using current chemical routes.

Specifically, the two companies are exploring the potential of the catalyst to produce chiral versions of derivatives through the reduction of beta keto esters and olefinic systems. Phoenix said it is already making use of GLFC's catalyst in some commercial applications.

Phoenix has developed a tube reactor system which will sit well with Ruthenium BINAP, according to Dr Phil Cotterill, GLFC's business development manager.

"The use of tube reactors and short residence times with this catalyst can have a dramatic and positive influence on the yield, quality and chiral integrity of the products formed," he said, adding that the collaboration "will result in improved process efficiencies, enhanced product quality and a reduction in manufacturing costs for a number of key intermediates."

80 per cent of all compounds in clinical development in the pharmaceutical industry are chiral, and marketed single-enantiomer agents racked up sales of $159 billion (€130bn) last year. Transition metal catalysts such as BINAP lie at the centre of their production, as they help shorten reaction times, have improved substrate to catalyst ratios and offer high enantioselectivity.

And the market for chiral tools is set to grow strongly, according to a study published earlier this year by Frost & Sullivan. Worldwide revenues due to chiral technology, which amounted to $4.8 billion in 1999, will more than triple to $14.9 billion by 2009, according to F&S.

Meanwhile, GFLC has entered into a partnership with High Force Research in which the latter will prepare a series of aryl substituted phenylalanines and derivatives for use as building blocks by pharma and biotech companies in drug screening programmes.

Successful candidates will be scaled up by High Force to provide gram to kilo quantities of material for drug development studies. When larger batches of product are required for clinical evaluation GLFC will scale-up the process for quantities ranging from multi-kilo to tonnes.

Initially, while the drugs are in their pre-clinical and clinical Phase I and II trials, the companies will use the GLFC asymmetric hydrogenation process technology to provide the chiral phenylalanines. However, as the volumes increase a switch will be made to produce the phenylalanines by proprietary bio-processes.