Subscribe to RSS
Please copy the URL and add it into your RSS Feed Reader.
https://www.thieme-connect.de/rss/thieme/en/10.1055-s-00000131.xml
Synfacts 2007(8): 0884-0884
DOI: 10.1055/s-2007-968811
DOI: 10.1055/s-2007-968811
Polymer-Supported Synthesis
© Georg Thieme Verlag Stuttgart · New York
C2-Aryl-PDB Library
D. Antonow, N. Cooper, P. W. Howard, D. E. Thurston*
Spirogen Limited, London and University of London, UK
Further Information
Publication History
Publication Date:
24 July 2007 (online)
Significance
A library of C2-arylated pyrrolo[2,1-c][1,4]benzodiazepines (PDB) was prepared through the Suzuki-Miyaura coupling of vinyl triflate 1 using a PS-supported palladium catalyst. Parallel reactions of the Suzuki-Miyaura coupling of 1 with a diverse set of boron reagents (66 examples) were carried out with a PS-supported palladium-phosphine complex under microwave conditions. After completion of the coupling reactions, N,N-diethanolaminomethyl polystyrene (PS-DEAM) was added to each reaction mixture to trap the unreacted boron reagent. The resulting mixtures were then subjected to parallel filtration through a phase separator cartridge to isolate the Suzuki products 2.