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Sigma-Aldrich and the University of Illinois Offer New Boronic Acid Surrogates to Researchers Worldwide Through Licensing Agreement
Date:10/7/2008

Technology expected to aid drug discovery by allowing for the rapid

synthesis of molecules using a single reaction

ST. LOUIS, Oct. 7 /PRNewswire-FirstCall/ -- Sigma-Aldrich (Nasdaq: SIAL) is pleased to announce that it has signed an exclusive licensing agreement with the University of Illinois at Urbana-Champaign allowing Sigma-Aldrich to offer research quantities of powerful new boronic acid surrogates for use in Suzuki-Miyaura coupling to researchers worldwide (http://sigma-aldrich.com/mida). Under the terms of the agreement, Sigma-Aldrich can also satisfy commercial-scale requests for these surrogates from its manufacturing customers.

Developed by Professor Martin Burke and co-workers, the technology has powerful implications for drug discovery, where the ability to quickly create large sets of related small molecules for use in screening is critical. The advancement relies on the use of a simple, low-cost, and environmentally-friendly ligand (N-methyliminodiacetic acid, "MIDA") that reversibly modulates boronic acids toward cross-coupling. The MIDA-ligated boronic acid building blocks can be used to construct target molecules using a single cross-coupling reaction in an iterative process, in a fashion resembling peptide synthesis. Complex bioactive molecules can also be efficiently constructed, as demonstrated in recent publications from the Burke research group in 2007 and 2008.

"Sigma-Aldrich has a nearly 40-year history of developing boron reagents for use by the chemical community, and we are delighted to maintain our leadership position in this area by garnering access to this potent technology," said Nate Wallock, Chemistry technology transfer manager at Sigma-Aldrich. "In collaboration with the Burke group, our R&D groups have actively developed the syntheses of dozens of MIDA boronic acid derivatives, many of which will be available globally in the comi
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