Intermediates for alpha-fluoroalkyl tetrabenazine and dihydrotetrabenazine imaging agents and probes
US7910738B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Nov 29, 2007 |
| Grant date | Mar 22, 2011 |
| Priority date | — |
| Expiry date | Oct 17, 2029 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D491/20
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention provides novel fluorophilic compounds having structure VIIwherein Q is a carbonyl group, a protected carbonyl group, a hydroxy methine group, or a protected hydroxy methine group; R1 is a C1-C20 aliphatic, C2-C20 cycloaliphatic, or C2-C20 aromatic radical comprising at least one functional group susceptible to reaction with nucleophilic fluoride ion or an electrophilic fluorinating agent; R2 is hydrogen or a C1-C10 aliphatic radical; and R3 is hydrogen or a C1-C10 aliphatic radical. The fluorophilic compounds are provided in both racemic and enantiomerically enriched forms and are useful as intermediates in the preparation of novel PET imaging agents and probes useful in the discovery and performance assessment of PET imaging agents. The fluorophilic compounds are particularly useful in the preparation of PET imaging agents and probes having a high affinity for VMAT-2, a biomarker implicated in human diabetes and other illnesses such as Parkinson's disease.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.