- Synthesis of achiral α,α-disubstituted β-alanines, and their use in construction of libraries of β-peptide conjugates of N-2-alkyl-1,2,3,4- tetrahydroisoquinolines on a solid support
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Six achiral N-phthaloyl protected α,α-disubstituted β-amino acids were synthesized, and used to construct a 96 compound library of 1,2,3,4- tetrahydroisoquinoline conjugates of β-peptides on a solid support. The library synthesis consisted of attachment of an appropriately 5-O-tethered 1,2,3,4-tetrahydroisoquinoline via the N-2 atom to a vinyl sulfonyl support, elongation of the deprotected 5-O-tether by repeated peptide coupling, quaternarization of N-2 with alkylamines and release of the β-peptide conjugate into solution with triethylamine.
- Heinonen, Petri,Virta, Pasi,Loennberg, Harri
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p. 7613 - 7624
(2007/10/03)
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