‘PharmaCore announced that it has acquired aromatic cross coupling technology from DSM Pharma Chemicals Venlo B.V. 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.

PharmaCore announced that it has acquired aromatic cross coupling technology from DSM Pharma Chemicals Venlo B.V. 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. 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, Ph.D., 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.

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