Unknown

Dataset Information

0

Synthesis of [(18) F] 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide (IDO5L): a novel potential PET probe for imaging of IDO1 expression.


ABSTRACT: To synthesize (18) F-labeled positron emission tomography (PET) ligands, reliable labeling techniques inserting (18) F into a target molecule are necessary. The (18) F-fluorobenzene moiety has been widely utilized in the synthesis of (18) F-labeled compounds. The present study utilized [(18) F]-labeled aniline as intermediate in [(18) F]-radiolabeling chemistry for the facile radiosynthesis of 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide ([(18) F]IDO5L) as indoleamine 2,3-dioxygenase 1 (IDO1) targeted tracer. IDO5L is a highly potent inhibitor of IDO1 with low nanomolar IC50 . [(18) F]IDO5L was synthesized via coupling [(18) F]3-chloro-4-fluoroaniline with carboximidamidoyl chloride as a potential PET probe for imaging IDO1 expression. Under the optimized labeling conditions, chemically and radiochemically pure (>98%) [(18) F]IDO5L was obtained with specific radioactivity ranging from 11 to 15?GBq/µmol at the end of synthesis within ~90?min, and the decay-corrected radiochemical yield was 18.2?±?2.1% (n?=?4).

SUBMITTER: Huang X 

PROVIDER: S-EPMC4655588 | biostudies-other | 2015 Apr

REPOSITORIES: biostudies-other

altmetric image

Publications

Synthesis of [(18) F] 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide (IDO5L): a novel potential PET probe for imaging of IDO1 expression.

Huang Xuan X   Gillies Robert J RJ   Tian Haibin H  

Journal of labelled compounds & radiopharmaceuticals 20150218 4


To synthesize (18) F-labeled positron emission tomography (PET) ligands, reliable labeling techniques inserting (18) F into a target molecule are necessary. The (18) F-fluorobenzene moiety has been widely utilized in the synthesis of (18) F-labeled compounds. The present study utilized [(18) F]-labeled aniline as intermediate in [(18) F]-radiolabeling chemistry for the facile radiosynthesis of 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide ([(18) F]IDO5L) as in  ...[more]

Similar Datasets

| S-EPMC2971256 | biostudies-other
| S-EPMC2983740 | biostudies-literature
| S-EPMC3011692 | biostudies-literature
| S-EPMC2960216 | biostudies-literature
| S-EPMC3601769 | biostudies-literature
| S-EPMC3344668 | biostudies-literature
| S-EPMC2967971 | biostudies-literature
| S-EPMC3407596 | biostudies-literature
| S-EPMC7044674 | biostudies-literature
| S-EPMC2960939 | biostudies-literature