Back to results
US 2019/0161435 A1Published application
Process for preparing acylated amphetamine derivatives
AssigneeSpecGX LLC
InventorsBrian Orr, Kevin Roesch, Joel McClenaghan
Life of this patent
Estimating the term…
Abstract
Processes for preparing acetylated amphetamine derivatives and, in particular, processes for preparing L-lysine-D-amphetamine dimesylate from D-amphetamine salts.
Claims20
A one-pot process for preparing a compound of Formula (IV), the process comprising:
- (a) forming a reaction mixture comprising a solvent and a compound of Formula (I), the solvent being an alkyl tetrahydrofuran;
- (b) adding a compound of Formula (II) to the reaction mixture, thereby forming an intermediate compound of Formula (III);
- (c) phase extracting the reaction mixture after step (b) with one or more aqueous solutions to remove the compounds of Formulas (I) and (II) and reaction by-products, thereby forming a purified mixture comprising the intermediate compound of Formula (III);
- and
- (d) contacting the purified mixture comprising the intermediate compound of Formula (III) with an acid to form the compound of Formula (IV);
- wherein:
- R is hydrocarbyl or substituted hydrocarbyl;
- LG is a leaving group;
- PG is a protecting group;
- and
- A is an anion.
8 more elements
A one-pot process for preparing L-lysine-D-amphetamine dimesylate, the process comprising:
- (a) converting a D-amphetamine salt to D-amphetamine;
- (b) adding D-amphetamine to a reaction mixture comprising 2-methyl tetrahydrofuran and N,N′-di-Boc-L-lysine hydroxysuccinimide ester to form an intermediate compound, the intermediate compound being N,N′-di-Boc-L-lysine-D-amphetamine;
- (c) phase extracting the reaction mixture after step (b) with one or more aqueous solutions to remove starting reactants and reaction by-products, thereby forming a purified mixture comprising the intermediate compound;
- and
- (d) contacting the purified mixture comprising the intermediate compound with methanesulfonic acid to form L-lysine-D-amphetamine dimesylate.
2 more elements
Dependencies are inferred from the claim text.