Synthesis and analysis of 2-[211At]- l-phenylalanine and 4-[211At]- l-phenylalanine and their uptake in human glioma cell cultures in-vitro

2-[211At]- l-phenylalanine and 4-[211At]- l-phenylalanine were prepared from the corresponding iodo and bromo derivatives using the Cu +-assisted nucleophilic exchange. 4-[211At]- l-phenylalanine was additionally prepared by destannylation of the BOC-derivatized 4-tributylstannyl- l-phenylalanine. R...

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Bibliographic Details
Published in:Applied radiation and isotopes 2010-06, Vol.68 (6), p.1060-1065
Main Authors: Meyer, Geerd J., Walte, Almut, Sriyapureddy, Siva R., Grote, Michaela, Krull, Doris, Korkmaz, Zekiye, Knapp, Wolfram H.
Format: Article
Language:English
Subjects:
Astatine
Brain Neoplasms - metabolism
Cell Line, Tumor
Cell uptake
Glioblastoma
Glioma - metabolism
Halogen exchange
Humans
Isotope Labeling - methods
Phenylalanine
Phenylalanine - analogs & derivatives
Phenylalanine - metabolism
Radiopharmaceuticals - metabolism
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Summary:2-[211At]- l-phenylalanine and 4-[211At]- l-phenylalanine were prepared from the corresponding iodo and bromo derivatives using the Cu +-assisted nucleophilic exchange. 4-[211At]- l-phenylalanine was additionally prepared by destannylation of the BOC-derivatized 4-tributylstannyl- l-phenylalanine. Radiochemical yields of 2-[211At]- l-phenylalanine and 4-[211At]- l-phenylalanine by nucleophilic exchange were 52–74% and 65–85%. Radiochemical yield of 4-[211At]- l-phenylalanine by electrophilic destannylation was 35–50%. HPLC sequence analysis showed that 2-[211At]- l-phenylalanine followed the halogen sequence (F
ISSN:0969-8043
1872-9800
DOI:10.1016/j.apradiso.2009.12.043