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Chemicals and biochemicals
News Release from: Pharmacore | Subject: Cross coupling technology
Edited by the Laboratorytalk Editorial
Team on 27 April 2005
The chemistry of cross-coupling
Proprietary chemistry allows aryl nitriles and aryl ethers to participate in cross coupling reactions to produce derivatives that are very useful in the manufacture of drugs and drug intermediates
PharmaCore has acquired aromatic cross coupling technology from DSM Pharma Chemicals Venlo, and is now the owner of this technology This proprietary chemistry allows a wide variety of aryl nitriles and aryl ethers to participate in cross coupling reactions to produce derivatives that are very useful in the manufacture of drugs and drug intermediates, including unsymmetrical biaryls, styrenes, alkylated aromatics, and alkynylated aromatics
This article was originally published on Laboratorytalk on 25 Jun 2003 at 8.00am (UK)
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Moreover, the acquisition also includes proprietary chemistry for the direct cross coupling of aryl Grignard reagents with functionally substituted aryl halides (including aryl chlorides).
This latter technology has been demonstrated previously at full production scale and offers an attractive alternative for scaling up traditional Suzuki coupling reactions.
"The unsymmetrical biaryl structural unit is exceedingly important in medicinal chemistry and, therefore, efficient means for its synthesis are crucial.
"This technology will give PharmaCore a distinct advantage in the production of certain unsymmetrical biaryl targets relative to current aryl halide based methodologies," said Joe Miller, vice president of chemistry at PharmaCore.
"In particular, certain classes of aryl nitriles and aryl ethers are significantly less expensive than the corresponding aryl halides, giving PharmaCore a real economic edge with respect to our competitors in the preparation of these target compounds".
The new aryl halide based cross coupling chemistry has been validated on full plant scale.
PharmaCore now offers customers the benefit of a proven, lower cost alternative to Suzuki couplings for pilot or larger scale production of unsymmetrical biaryl compounds.
PharmaCore, headquartered in High Point, NC, describes itsef as a rapidly emerging leader in small molecule chemistry for drug discovery.
The company develops and manufactures novel chemical building blocks and scaffolds for drug-like molecules, provides custom synthesis services (including GMP scale-up) of pharmaceutical intermediates and APIs, and performs contract research to support drug discovery efforts at major pharmaceutical and biotechnology companies.
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