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
Abstract
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:
- Research Org.:
- Univ. of California (United States)
- OSTI Identifier:
- 27714
- Patent Number(s):
- 5393908
- Application Number:
- PAN: 7-903,915; CNN: Grant PO1-NS-15654;Grant RO1-MH-37916
- Assignee:
- PTO; SCA: 550601; PA: EDB-95:059845; SN: 95001354447
- DOE Contract Number:
- FC03-87ER60615
- Resource Type:
- Patent
- Resource Relation:
- Other Information: PBD: 28 Feb 1995
- Country of Publication:
- United States
- Language:
- English
- Subject:
- 55 BIOLOGY AND MEDICINE, BASIC STUDIES; RADIOPHARMACEUTICALS; CHEMICAL PREPARATION; FLUORINE 18; LIQUID COLUMN CHROMATOGRAPHY; NUCLEAR MEDICINE
Citation Formats
Satyamurthy, N, Barrio, J R, Bishop, A J, and Namavari, M. 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. United States: N. p., 1995.
Web.
Satyamurthy, N, Barrio, J R, Bishop, A J, & Namavari, M. 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. United States.
Satyamurthy, N, Barrio, J R, Bishop, A J, and Namavari, M. Tue .
"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". United States.
@article{osti_27714,
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},
author = {Satyamurthy, N and Barrio, J R and Bishop, A J and Namavari, M},
abstractNote = {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.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {1995},
month = {2}
}
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