TY - JOUR
T1 - A new Heck reaction modification using ketone Mannich bases as enone precursors
T2 - Parallel synthesis of anti-leishmanial chalcones
AU - Reichwald, Christina
AU - Shimony, Orly
AU - Sacerdoti-Sierra, Nina
AU - Jaffe, Charles L.
AU - Kunick, Conrad
N1 - Funding Information:
Funding by a grant of the European Commission (Contract No. LSHB-CT-2004-503467; to C.R., C.L.J., and C.K.) is gratefully acknowledged.
PY - 2008/3/15
Y1 - 2008/3/15
N2 - A new Heck-type reaction for the synthesis of chalcones has been established using Mannich bases as enone precursors. The novel reaction proceeds rapidly in air atmosphere under ligandless conditions and can be adapted for library synthesis in a parallel reactor station. Screening of the synthesized chalcones revealed N-{4-[(1E)-3-oxo-3-(3-pyridinyl)-1-propenyl]phenyl}benzamide (3f) to be a potent anti-leishmanial agent.
AB - A new Heck-type reaction for the synthesis of chalcones has been established using Mannich bases as enone precursors. The novel reaction proceeds rapidly in air atmosphere under ligandless conditions and can be adapted for library synthesis in a parallel reactor station. Screening of the synthesized chalcones revealed N-{4-[(1E)-3-oxo-3-(3-pyridinyl)-1-propenyl]phenyl}benzamide (3f) to be a potent anti-leishmanial agent.
KW - Chalcones
KW - Heck reaction
KW - Leishmania
UR - http://www.scopus.com/inward/record.url?scp=40749144801&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2008.01.112
DO - 10.1016/j.bmcl.2008.01.112
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C2 - 18276134
AN - SCOPUS:40749144801
SN - 0960-894X
VL - 18
SP - 1985
EP - 1989
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 6
ER -