TY - JOUR
T1 - Reductive N-alkylation of secondary amines with [2-11C]acetone
AU - Van Der Meij, Margaretha
AU - Carruthers, Nicholas I.
AU - Herscheid, Jacobus D M
AU - Jablonowski, Jill A.
AU - Leysen, Josee E.
AU - Windhorst, Albert D.
PY - 2003/10/1
Y1 - 2003/10/1
N2 - The development of a labeling method for secondary amines with [2- 11C]acetone is described since the R2N-isopropyl moiety is present in many biologically active compounds. The influence of a variety of parameters (e.g. reagents, solvents, temperature, and time) on the reaction outcome is discussed. Under the optimal reaction conditions, [ 11C]1-isopropyl-4-phenylpiperazine ([11C]iPPP) was synthesized from [2-11C]acetone and 1-phenylpiperazine in a decay-corrected radiochemical yield of 72%. The overall synthesis time, from EOB to HPLC analysis of [11C]iPPP, was 20 min. Specific activity was 142-208 GBq/μmol at the end of synthesis.
AB - The development of a labeling method for secondary amines with [2- 11C]acetone is described since the R2N-isopropyl moiety is present in many biologically active compounds. The influence of a variety of parameters (e.g. reagents, solvents, temperature, and time) on the reaction outcome is discussed. Under the optimal reaction conditions, [ 11C]1-isopropyl-4-phenylpiperazine ([11C]iPPP) was synthesized from [2-11C]acetone and 1-phenylpiperazine in a decay-corrected radiochemical yield of 72%. The overall synthesis time, from EOB to HPLC analysis of [11C]iPPP, was 20 min. Specific activity was 142-208 GBq/μmol at the end of synthesis.
KW - Reductive alkylation
KW - Reductive amination
KW - Secondary amines
KW - [2-C]acetone
KW - [2-C]tert-butanol
UR - http://www.scopus.com/inward/record.url?scp=0242408779&partnerID=8YFLogxK
U2 - https://doi.org/10.1002/jlcr.740
DO - https://doi.org/10.1002/jlcr.740
M3 - Article
SN - 0362-4803
VL - 46
SP - 1075
EP - 1085
JO - Journal of Labelled Compounds and Radiopharmaceuticals
JF - Journal of Labelled Compounds and Radiopharmaceuticals
IS - 11
ER -