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18F - Fluciclovine compositions in citrate buffers
专利权人:
GE Healthcare LIMITED
发明人:
Kristine Romoren,Olav Ryan
申请号:
GB201810553
公开号:
GB2561122A
申请日:
2012.12.21
申请国别(地区):
GB
年份:
2018
代理人:
摘要:
Claimed is a method for obtaining a radiopharmaceutical composition of 18F-1-amino-3-fluoro-cyclobutane-1-carboxylic acid (18F-FACBC) where said composition comprises; 50-100 mM citrate buffer and has a pH of 4.0-5.0 and wherein said method comprises: (i) reacting with a suitable source of [18F] a compound of formula (I) (where LG is a leaving group, PG1 is a carboxy protecting group and PG2 is an amine protecting group) to obtain a compound of wherein the leaving group has been replaced with 18F, (ii) removal of PG1, (iii) removal of PG2 to obtain crude 18F FACBC, (iv) carrying out a purification step comprising passing said crude product through a hydrophilic lipophilic balanced (HLB) solid phase to obtain ­18F FACBC, (v) formulating said 18F-FACBC with citrate buffer. Preferably, the composition comprises 60-90 mM citrate buffer. Preferably, the composition has a pH of 4.1-4.5. Formula (I)
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