Process for the preparation of radioiodinated 3-fluoropropyl-nor-β-CIT
AssigneeMallinckrodt Inc.
InventorEdmund C. Hudson
Life of this patent
Estimating the term…
Abstract
The invention generally provides processes for the preparation of radioiodinated 3-fluoropropyl-nor-β-CIT. In particular, the process uses an arylsilane intermediate, thus avoiding the use of hexamethylditin, and reducing the number of steps previously required for the preparation of radioiodinated 3-fluoropropyl-nor-β-CIT from anhydroecgonine methyl ester. The invention also relates to the alkylation of a nortropane to the corresponding N-(3-fluoropropyl) analog using 3-fluoropropanal.
Claims16
A process for the preparation of compound (I) comprising the following reaction scheme:
- wherein:
- X is a halogen, and
- Me is methyl;
- and
- wherein the alkylating agent is 3-fluoropropanol.
A process for the preparation of a N-(3-fluoropropyl) compound (III), the process comprising contacting a nortropane compound (II) with 3-fluoropropanol in the presence of a reducing agent to form compound (III):
- wherein R1 is selected from the group consisting of halogen, Si(CH3)3, and Sn(CH3)3.
Dependencies are inferred from the claim text.