ClTi (OiPr) 3-promoted reductive amination on the solid phase: combinatorial synthesis of a biaryl-based sulfonamide library

Gutierrez, C.D.; Bavetsias, V.; McDonald, E.

Journal of Combinatorial Chemistry 10(2): 280-284


ISSN/ISBN: 1520-4766
PMID: 18189368
DOI: 10.1021/cc700132f
Accession: 052094267

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A combinatorial library (9 amines x 7 sulfonyl chlorides x 13 boronic acids = 819 compounds) was produced on solid support in a four-step sequence, i.e., ClTi(O(i)Pr)3-promoted reductive amination, sulfonylation of the resin-bound amine, Suzuki cross-coupling, and acid-mediated cleavage. The library members were obtained in moderate quantity (1-8 mg) with over 70% of the sampled products greater than 90% pure according to LC-MS analysis.