A new multi-gram synthetic route to labeling precursors for the D(2/3) PET agent 18F-fallypride.
This Letter describes a new multi-gram synthetic protocol for the preparation of the classic tosylate labeling precursor for the D(2/3) PET agent [(18)F]fallypride. In the course of our studies, we also discovered two novel labeling precusors, the previously undescribed mesylate and chloro congeners of fallypride.
Kim
Kwangho
K
Department of Chemistry and Pharmacology, Institute of Chemical Biology, Vanderbilt University, 802 Robinson Research Building, Nashville, TN 37235-1822, USA.
Miller
Nicole R
NR
Sulikowski
Gary A
GA
Lindsley
Craig W
CW
D001549:Benzamides / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002713:Chlorine / Q000737:chemistry; D065127:Dopamine D2 Receptor Antagonists; D015195:Drug Design; D008698:Mesylates / Q000737:chemistry; D008956:Models, Chemical; D049268:Positron-Emission Tomography / Q000295:instrumentation* / Q000379:methods; D011759:Pyrrolidines / Q000494:pharmacology*; D019275:Radiopharmaceuticals / Q000494:pharmacology*; D017448:Receptors, Dopamine D2 / Q000737:chemistry; D050637:Receptors, Dopamine D3 / Q000037:antagonists & inhibitors / Q000737:chemistry
D001549:Benzamides; D065127:Dopamine D2 Receptor Antagonists; D008698:Mesylates; C094948:N-((1-allyl-2-pyrrolidinyl)methyl)-5-(3-fluoropropyl)-2,3-dimethoxybenzamide; D011759:Pyrrolidines; D019275:Radiopharmaceuticals; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; D002713:Chlorine