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
Patent
·
OSTI ID:27714
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.
- Research Organization:
- University of California
- DOE Contract Number:
- FC03-87ER60615
- Assignee:
- PTO; PA: EDB-95:059845; SN: 95001354447; SCA: 550601
- Patent Number(s):
- US 5,393,908/A/
- Application Number:
- PAN: 7-903,915; CNN: Grant PO1-NS-15654; Grant RO1-MH-37916
- OSTI ID:
- 27714
- Country of Publication:
- United States
- Language:
- English
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