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
US5393908A · kind A · utility
3Cited by
2References
12Claims
0Family size
Inventors
Key dates
| Filing date | Jun 25, 1992 |
| Grant date | Feb 28, 1995 |
| Priority date | — |
| Expiry date | Jun 25, 2012 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F7/2208
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.