Buchwald 4th generation palladcycles

Buchwald 4th generation palladcycles

 

Strem  Chemicals

Buchwald Ligands and precatalysts

UK is able to offer products from this newest generation of palladacycles

 

Many of our kits are used in Pharma research and contain a variety of chemicals commonly combined when screening experiments

We have provided a wide range of Buchwald ligands and Precatalysts for nearly 20 years. Our license allows us to provide this technology for R&D and commercial applications. We have continued to add to this product line in order to better serve our customers and allow them to achieve their research and commercial objectives.

Strem is now pleased to provide further advancement in Buchwald Palladacycle technology by offering a 4th generation as “N-methyl” analogues of the catalysts’ 2-aminobiphenyl moiety.  Whereas the 2nd and 3rd generation Buchwald Precatalysts fostered significant advances in organic syntheses and produced high yields with a wide variety of substrates, they were based on the 2-aminobiphenyl ligand.  However, the primary amino group in the ligand can lead to synthetic limitations, especially in a pharmaceutical environment.

Upon activation of the catalyst, the 2-aminobiphenyl converts mainly into carbazole, a secondary amine that itself can serve as a substrate in the coupling reactions of amines with aryl halides.  This side reaction can consume valuable starting material and lead to complications in purification.  Buchwald 4th generation Precatalysts based on N-methyl biphenyl will produce N-methyl carbazole upon activation, which cannot act as substrate in these types of reactions. Another drawback from 3rd generation Precatalysts is remaining traces of 2-aminobiphenyl in the product. Aminobiphenyls have been associated with carcinogenicity (4-aminobiphenyl is a known carcinogen); therefore, its absence is desirable, especially in pharmaceutical syntheses.

Our most famous items are the seven Buchwald kits including the most recent, a generation 4 Buchwald Palladacycle Precatalyst Kit 4, (Methanesulfonato-2′-methylamino-1, 1’-biphenyl-2-yl- Palladacycles

Our new booklet is available either on the web or buying emailing enquiries@www.strem.co.uk