Library of biphenyl privileged substructures using a safety-catch linker approach
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Library of biphenyl privileged substructures using a safety-catch linker approach. / Severinsen, Rune; Bourne, Gregory T; Tran, Tran T; Ankersen, Michael; Begtrup, Mikael; Smythe, Mark L.
I: Journal of Combinatorial Chemistry, Bind 10, Nr. 4, 2008, s. 557-566.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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TY - JOUR
T1 - Library of biphenyl privileged substructures using a safety-catch linker approach
AU - Severinsen, Rune
AU - Bourne, Gregory T
AU - Tran, Tran T
AU - Ankersen, Michael
AU - Begtrup, Mikael
AU - Smythe, Mark L
N1 - Keywords: Biphenyl Compounds; Catalysis; Combinatorial Chemistry Techniques; Cross-Linking Reagents; Molecular Structure
PY - 2008
Y1 - 2008
N2 - A biphenyl privileged structure library containing three attachment points were synthesized using a catechol-based safety-catch linker strategy. The method requires the attachment of a bromo-acid to the linker, followed by a Pd-catalyzed Suzuki cross-coupling reaction. Further derivatization, activation of the linker with strong acid and aminolysis afforded the respective products in high purity and good overall yield. To show the versatility of the synthesis, a 199-member library was generated. The library samples both conformational and chemical diversity about a well-known privileged substructure.
AB - A biphenyl privileged structure library containing three attachment points were synthesized using a catechol-based safety-catch linker strategy. The method requires the attachment of a bromo-acid to the linker, followed by a Pd-catalyzed Suzuki cross-coupling reaction. Further derivatization, activation of the linker with strong acid and aminolysis afforded the respective products in high purity and good overall yield. To show the versatility of the synthesis, a 199-member library was generated. The library samples both conformational and chemical diversity about a well-known privileged substructure.
KW - Former Faculty of Pharmaceutical Sciences
U2 - 10.1021/cc800006g
DO - 10.1021/cc800006g
M3 - Journal article
C2 - 18462009
VL - 10
SP - 557
EP - 566
JO - ACS Combinatorial Science
JF - ACS Combinatorial Science
SN - 2156-8952
IS - 4
ER -
ID: 10113426