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Title: Synthesis of N-formyl-3,4-di-t-butoxycarbonyloxy-6(trimethylstannyl)-L-phenylalanine ethyl ester and its regioselective radiofluorodestannylation to 6-[{sup 18}F]fluoro-L-dopa

A protected 6-trimethylstannyl dopa derivative has been synthesized for the as a precursor for the preparation of 6-[{sup 18}F]fluoro-L-dopa. The tin derivative readily reacts with electrophilic radiofluorinating agents such as [{sup 18}F]F{sub 2}, [{sup 18}F]OF{sub 2} and [{sup 18}F]AcOF. The [{sup 18}F]fluoro intermediate was easily hydrolyzed with HBr and the product 6-[{sup 18}F]fluoro-L-dopa was isolated after HPLC purification in a maximum radiochemical yield of 23%, ready for human use. 1 fig.
Inventors:
; ; ;
Issue Date:
OSTI Identifier:
27714
Assignee:
PTO; SCA: 550601; PA: EDB-95:059845; SN: 95001354447
Patent Number(s):
US 5,393,908/A/
Application Number:
PAN: 7-903,915; CNN: Grant PO1-NS-15654;Grant RO1-MH-37916
Contract Number:
FC03-87ER60615
Resource Relation:
Other Information: PBD: 28 Feb 1995
Research Org:
University of California
Country of Publication:
United States
Language:
English
Subject:
55 BIOLOGY AND MEDICINE, BASIC STUDIES; RADIOPHARMACEUTICALS; CHEMICAL PREPARATION; FLUORINE 18; LIQUID COLUMN CHROMATOGRAPHY; NUCLEAR MEDICINE

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