Palladium-mediated conversion of para-aminoarylboronic esters into para-aminoaryl- 11C-methanes
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Palladium-mediated conversion of para-aminoarylboronic esters into para-aminoaryl- 11C-methanes. / Andersen, Valdemar Lykke; Herth, Matthias Manfred; Lehel, Szabolcs; Knudsen, Gitte Moos; Kristensen, Jesper Langgaard.
In: Tetrahedron Letters, Vol. 54, No. 3, 2013, p. 213-216.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Palladium-mediated conversion of para-aminoarylboronic esters into para-aminoaryl- 11C-methanes
AU - Andersen, Valdemar Lykke
AU - Herth, Matthias Manfred
AU - Lehel, Szabolcs
AU - Knudsen, Gitte Moos
AU - Kristensen, Jesper Langgaard
PY - 2013
Y1 - 2013
N2 - Cross-couplings are an alternative to conventional 11C-methylations which are generally employed in PET tracer synthesis. Therefore, we set out to develop a general procedure for the synthesis of para-11CH3 labeled aromatic amines from the corresponding para-aminoarylboronic esters in the presence of free amines. Aryl boronic esters containing primary, secondary, and tertiary amines were successfully converted into corresponding labeled methyl derivatives in suf¿cient radiochemical yield to apply thismethod for tracer development. This procedure was applied to the labeling of CIMBI-712, a promisingcandidate for the in vivo imaging of the 5-HT 7 receptor in the CNS
AB - Cross-couplings are an alternative to conventional 11C-methylations which are generally employed in PET tracer synthesis. Therefore, we set out to develop a general procedure for the synthesis of para-11CH3 labeled aromatic amines from the corresponding para-aminoarylboronic esters in the presence of free amines. Aryl boronic esters containing primary, secondary, and tertiary amines were successfully converted into corresponding labeled methyl derivatives in suf¿cient radiochemical yield to apply thismethod for tracer development. This procedure was applied to the labeling of CIMBI-712, a promisingcandidate for the in vivo imaging of the 5-HT 7 receptor in the CNS
U2 - 10.1016/j.tetlet.2012.11.001
DO - 10.1016/j.tetlet.2012.11.001
M3 - Journal article
VL - 54
SP - 213
EP - 216
JO - Tetrahedron Letters
JF - Tetrahedron Letters
SN - 0040-4039
IS - 3
ER -
ID: 43227214