Improved synthesis of anti-[18F]FACBC: improved preparation of labeling precursor and automated radiosynthesis.
The non-natural amino acid anti-1-amino-3-[18F]fluorocyclobutyl-1-carboxylic acid (FACBC) has shown promise for tumor imaging with positron emission tomography. An improved synthesis of the precursor of anti-[18F]FACBC has been devised which demonstrates high stereoselectivity and suitability for large-scale preparations. An automated radiosynthesis has been developed which provides anti-[18F]FACBC in 24% decay-corrected yield. Additionally, the major non-radioactive species present in doses of anti-[18F]FACBC has been identified as anti-1-amino-3-hydroxycyclobutane-1-carboxylic acid. Together, these results are important steps towards the routine production of anti-[18F]FACBC for human use.
McConathy
Jonathan
J
Department of Radiology, EUH, Emory University, 1364 Clifton Road NE, Atlanta, GA 30322, USA.
Voll
Ronald J
RJ
Yu
Weiping
W
Crowe
Ronald J
RJ
Goodman
Mark M
MM
D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000302:isolation & purification*; D003503:Cyclobutanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000302:isolation & purification*; D006801:Humans; D007553:Isotope Labeling / Q000379:methods*; D009369:Neoplasms / Q000000981:diagnostic imaging / Q000378:metabolism; D011786:Quality Control; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry / Q000302:isolation & purification; D014055:Tomography, Emission-Computed / Q000379:methods
D002264:Carboxylic Acids; D003503:Cyclobutanes; D019275:Radiopharmaceuticals; C117460:fluciclovine F-18